34 results about "DESOXY" patented technology

Synthesis of N4-acyl-5,-deoxidation-5-fluorine cytidine is carried out by inducing dual-carbonic ether as sugar-structured hydroxyl into protective intra-annular ester acidating agent, taking 5,-deoxidation-5-fluorine cytidine(compound II) as initial raw material, and reacting intermediate compound(III) and with compound(IV) by three-step method to obtain final product. It is simple, has more yield and short reactive time. It can be used for industrial production.

The invention provides a 4'-desoxy-4'-alkylated or acylated amino substituted avermectin B2a / 2b derivative which is an alkylated or acylated avermectin B2a / 2b amino derivative synthesized by using methylamino avermectin B2a / 2b as a matrix. The 4'-desoxy-4'-alkylated or acylated amino substituted avermectin B2a / 2b derivative widens the utilization range of avermectin B2a / 2b, enhances the disinsection effect of the avermectin B2a / 2b and effectively prolongs the duration time of the product. The invention also provides a preparation method of the 4'-desoxy-4'-alkylated or acylated amino substituted avermectin B2a / 2b derivative and application of the 4'-desoxy-4'-alkylated or acylated amino substituted avermectin B2a / 2b derivative in preparing preparations for controlling pests of plants and animals.

The invention discloses novel N-4-phenylsulfonamido--N'-1-desoxy-(2-desoxy-2-substituted-amino)-beta-D-glucopyransoylthiocarbamide compounds with the general formula disclosed in the specification, which have the activity of inhibiting carbonic anhydrase and further achieve the effect of resisting tumor metastasis and invasion. The compounds structurally have the three active segments sulfamine, substituted glucosamine and thiocarbamide, and the three active segments and Zn<2+> ions in the carbonic anhydrase form coordinate bonds, thereby inhibiting the catalytic activity of the enzyme and performing the function of resisting tumor metastasis and invasion. Thus, the compounds have application potential in the aspect of antitumor drugs. In the general formula, R is defined in the specification.

The invention relates to a preparation method of 2'3'-di-O-acetyl-5'-desoxy-5-fluoro-N4-(pentyloxycarbonyl)cytidine, belonging to the technical field of medicine. The compound is an important intermediate of Capecitabine. The preparation method comprises the following step: by using anhydrous sodium carbonate or anhydrous potassium carbonate as alkali, quaternary ammonium salt as a phase-transfer catalyst and 4-substituted-pyridine as a catalyst, carrying out amidation reaction on 2'3'-di-O-acetyl-5'-desoxy-5-fluorocytidine and amyl chloroformate to obtain the 2'3'-di-O-acetyl-5'-desoxy-5-fluoro-N4-(pentyloxycarbonyl)cytidine. The invention adopts the anhydrous sodium carbonate or anhydrous potassium carbonate instead of the high-toxicity organic alkali pyridine, and obtains ideal yield and product purity. The method has the advantages of accessible raw materials, low cost, small environmental hazard, high safety and reliability, short reaction time and good product quality.

The invention relates to a method for manufacturing rollers by using high-speed steel. The method includes processing steps that ordinary metals are mixed according to a ratio and added into an electric furnace to be heated and molten; ingredients are regulated up to standard before being put into the furnace and heated to 1580 DEG C to 1630 DEG C, and Al deoxidation and alloying accounting for 0.3% to 0.8% of molten steel is added; gray iron or ductile iron is used for casting, the gray iron or ductile iron is preheated to 230 DEG C to 240 DEG C, and fireproof paints are coated on the inner surface; the temperature of the molten iron is adjusted to 1510 DEG C to 1550 DEG C, and a centrifugal machine is started; an annealing process is that casting blanks are heated to 700 DEG C to 750 DEG C along with a heat treatment furnace with a temperature no less than 200 DEG C; and quenching is performed after rough machining. According to the method, manufactured rollers are fine and uniform in structure, high in strength and toughness and good in thermal fatigue resistance; and cracks, stripping and roller crushing during the usage of the rollers cannot occur.

The invention discloses a beta-cyclodextrin derivative and a preparation method and application thereof. The beta-cyclodextrin derivative is a single [6-(2-hydroxy ethyl) amino-6-desoxy]-beta-cyclodextrin, single [6-di(2-hydroxy ethyl) amino-6-desoxy]-beta-cyclodextrin, single [6-(2-hydroxy propyl) amino-6-desoxy]-beta-cyclodextrin, single [ 6 di(2-hydroxy propyl ) amino-6- desoxy]-beta-cyclodextrin, single [6-(3-hydroxy propyl) amino-6-desoxy)-beta-cyclodextrin, single [6-methyl ( 2-hydroxy ethyl ) amino-6-desoxy]-beta-cyclodextrin, single {6- [(2S)-2-hydroxy propyl] amino-6-desoxy}-beta-cyclodextrin and single {6[(2R)-2-hydroxy propyl] amino-6- desoxy}-beta- yclodextrin. The beta-cyclodextrin derivative can be prepared by a nucleophilic substitution reaction of single (6-O-p-toluene sulfonyl)-beta-cyclodextrin and corresponding aminoalcohol. The synthesis method has the advantages of simple operation, mild reaction conditions, simple purification, high yield and good purity of object products. The beta-cyclodextrin derivative can be used as a water-soluble ligand of metal mimic enzyme in aqueous metallic catalytic oxidation and aqueous metallic catalytic reduction reaction.

The invention relates to a glucosamine-containing 1,3,4-thiadiazole derivative and a synthesis method of the lucosamine-containing 1,3,4-thiadiazole derivative. The method comprises the following steps: reacting 2-desoxy-2-isorhodanate-1,3,4,6-tetra-O-benzyl-beta-D-glucopyranose with hydrazine hydrate to synthesize an intermediate glycosyl thiosemicarbazide, and reacting with substituted aldehyde and a Fe<3+> compound to synthesize the N-(5-substituted-1,3,4-thiadiazolyl-2-yl)-1,3,4,6-tetra-O-benzyl-2-desoxy-beta-D-glucosamine. The synthesis method is simple and safe to operate, and has the advantages of small environmental pollution, high yield and simple after-treatment. The synthesized compound has a strong inhibiting effect on acetylcholinesterase, and has wide application prospects in the aspect of preparation of anti-acetylcholinesterase drugs.

The invention belongs to the technical field of chemical medicines, and particularly relates to a Beta-L-2'-desoxy-thymine nucleoside derivative, a preparation method and purposes thereof. The Beta-L-2'-desoxy-thymine nucleoside derivative has a structure as showed in a format I, wherein R1 and R2 are independent O, S or Se; when one of the R1 and the R2 is O, R3 is halogen, -OH, -NH2, C1-C8 alkyl, (CH2)nF, (CH2)n-1CHF or CF3; R4 is halogen, H, or CF3; and n is 1-8. The invention provides the derivative which has activity of resisting hepatitis virus, and offers a new choice for preparing medicines capable of treating the hepatitis.

Conjugates of transferrin, albumin and polyethylence glycol consisting of native or thiolated transferrin or albumin or of polyethylene glycol (MW between approximately 5,000 and 20,0000) with at least one HS-, HO- or H2N group and cytostatic compounds derived through maleinimide or N-hydroxysuccinimide ester compounds, such as doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxandrone, chloroambucil, melphalan, 5-fluorouracyl, 5'-desoxy-5-fluorouridine, thioguanine, methotrexate, paclitaxel, docetaxel, topotecan, 9-aminocamptothecin, etoposide, teniposide, mitopodoside, vinblastine, vincristine, vindesine, vinorelbine or a compound of general formula A, B, C or D, where n=0-6, X=-NH2, -OH, -COOH, -O-CO-R-COR*, -NH-CO-R-COR*, where R is an aliphatic carbon chain with 1-6 carbon atoms or a substituted or unsubstituted phenylene group and R*H, phenyl, alkyl with 1-6 carbon atoms.

Compositions and methods to improve the cleaning performance of washing agents during laundering of textiles are disclosed. Compositions described use 6-desoxy-6-amino-celluloses. Methods for laundering textiles, in which a detergent and a soil release active ingredient are used in the form of a cellulose derivative as defined above, are also included. These methods can be performed manually or as appropriate with the aid of a conventional domestic washing machine.

The invention discloses a method for making aluminum ion fluorescent detection based on selective aluminum cation recognizing and binding of 2-desoxy-2- [(E)-[2-hydroxyl-1-2-hydroxyl-1-naphthoicmethylene]amino] -D-glucose compound obtained by condensation of naphthoic aldehyde and D-glucosamine, where the compound can make high-selectivity aluminum ion fluorescent detection, and can obviously detect aluminum ion concentration down to 0.013ppm, without interferences of other ions such as Li(I),Na(I),K(I),Ag(I),Mg(II),Ca(II),Cu(II),Ba(II),Pb(II),Mn(II),Co(II),Ni(II),Cd(II),Zn(II) and Hg(II). And it provides a method for detecting aluminum ions in water sample in high selectivity and high sensitivity.

The invention discloses a Streptomyces-carpaticus-derived marine microbial polysaccharide and a preparation method thereof. According to the invention, the marine-derived Streptomyces carpaticus OUCMDZ-726 is fermented to prepare the marine microbial polysaccharide in novel chemical structure, which is a linear homopolymer formed by connecting 3-desoxy-D-glycerol-D-ganonulose with alpha-2,8. The marine microbial polysaccharide has unique structure, is derived from marine microbes, can be used for producing and researching precursors or intermediates of novel drugs, and thus, can be fully utilized; and the functions and activities of the marine microbial polysaccharide can be widely developed.

The invention relates to an enzyme from Bailing production bacterium Cordyceps Chinese Hirsutella for synthesizing metabolic (desoxy) uridine from (desoxy) cytidine, a gene for coding the enzyme and application thereof. The enzyme is cytidine deaminase which has more than 90% of homology with amino acid sequence disclosed as SEQ ID NO.1; and the coding gene has more than 90% of homology with nucleotide sequence disclosed as SEQ ID NO.2. The invention researches the metabolic pathway of (desoxy) cytidine synthesized (desoxy) uridine in details in principle. The cloned DNA (deoxyribonucleic acid) comprising the nucleotide sequence provided by the invention can be transformed into engineering bacterium by transduction, conversion and conjugal transfer. By adjusting the expression of the (desoxy) uridine biosynthesized gene, the host (desoxy) uridine is endowed with high expressivity, thereby providing an effective way for enhancing the yield of the (desoxy) uridine and having great application prospects.

The invention discloses a specific monoclonal antibody capable of distinguishing mequindox and olaquindox metabolites, and an enzyme-linked immunosorbent assay method and kit for detecting the mequindox and olaquindox metabolites. According to the invention, the monoclonal antibody is secreted by a hybridoma cell strain DMEQ1A3 of which the preservation number is CCTCC N0.C201496. Compared with the prior art, the monoclonal antibody prepared by the invention can distinguish desoxy mequindox and desoxy olaquindox at the same time, and has higher sensitivity and specificity. The ELISA method and the kit, disclosed by the invention, can detect the residue of the mequindox and olaquindox metabolites in meat food at the same time, and have the advantages of high detection efficiency, high sensitivity, high precision, high accuracy and the like.

The invention relates to an enzyme from Bailing production bacterium Cordyceps Chinese Hirsutella for synthesizing metabolic (desoxy) uridine from (desoxy) cytidine, a gene for coding the enzyme and application thereof. The enzyme is cytidine deaminase which has more than 90% of homology with amino acid sequence disclosed as SEQ ID NO.1; and the coding gene has more than 90% of homology with nucleotide sequence disclosed as SEQ ID NO.2. The invention researches the metabolic pathway of (desoxy) cytidine synthesized (desoxy) uridine in details in principle. The cloned DNA (deoxyribonucleic acid) comprising the nucleotide sequence provided by the invention can be transformed into engineering bacterium by transduction, conversion and conjugal transfer. By adjusting the expression of the (desoxy) uridine biosynthesized gene, the host (desoxy) uridine is endowed with high expressivity, thereby providing an effective way for enhancing the yield of the (desoxy) uridine and having great application prospects.

This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.

This invention discloses 3-desoxy-2-methylene-vitamin D analogs, and specifically (20S)-3-desoxy-1α,25-dihydroxy-2-methylene-vitamin D3 and (20R)-3-desoxy-1α, 25-dihydroxy-2-methylene-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.

The invention discloses complexes formed by 6-[(1,2,3,4-tetrahydro-beta-carbolinyl-3)-formacyl-diethylenetriamino]-6-desoxy-beta-cyclodextrin (formed by connecting tetrahydro-beta-carbolinylcarboxylic acid to cyclodextrin by using diethylenetriamine as a connecting arm) and copper and a preparation method thereof. The invention further discloses favorable in-vivo antithrombotic activity and in-vitro vasodilatation action of the copper complexes. The invention provides excellent candidate compounds for developing medicines with high bioavailability and strong antithrombotic activity.

The invention discloses a synthesis method of 9-desoxy-9-homoerythromycin A(Z) oxime, which comprises the following steps: adding 9-desoxy-9-homoerythromycin A(E) oxime into an organic solvent, wherein the mass-volume ratio of the 9-desoxy-9-homoerythromycin A(E) oxime to the organic solvent is 1g:(3-10)ml; stirring until the 9-desoxy-9-homoerythromycin A(E) oxime is completely dissolved, and adding an alkali, wherein the mole ratio of the 9-desoxy-9-homoerythromycin A(E) oxime to the alkali is 1:(0.2-1.0); stirring at 0-5 DEG C for 64-82 hours; and after the reaction finishes, filtering, washing the obtained filter residue with a 0-5-DEG C organic solvent to obtain a white solid, and carrying out vacuum drying on the white solid to obtain the 9-desoxy-9-homoerythromycin A(Z) oxime finished product. The method is very simple in technical process and very convenient to operate. The synthesized 9-desoxy-9-homoerythromycin A(Z) oxime has the advantages of high purity, no color change and high yield.

The invention relates to an enzyme from Bailing production bacterium Cordyceps Chinese Hirsutella for synthesizing metabolic (desoxy) pyrimidine nucleoside triphosphate from (desoxy) pyrimidine nucleoside diphosphate, a gene for coding the enzyme and application thereof. The enzyme is nucleoside diphosphokinase which has more than 90% of homology with amino acid sequence disclosed as SEQ ID NO.1; and the coding gene has more than 90% of homology with nucleotide sequence disclosed as SEQ ID NO.2. The invention researches the metabolic pathway of (desoxy) pyrimidine nucleoside diphosphate synthesized (desoxy) pyrimidine nucleoside triphosphate in details in principle. The cloned DNA (deoxyribonucleic acid) comprising the nucleotide sequence provided by the invention can be transformed into engineering bacterium by transduction, conversion and conjugal transfer. By adjusting the expression of the (desoxy) pyrimidine nucleoside triphosphate biosynthesized gene, the host (desoxy) pyrimidine nucleoside triphosphate is endowed with high expressivity, thereby providing an effective way for enhancing the yield of the (desoxy) pyrimidine nucleoside triphosphate and having great application prospects.

The invention relates to an enzyme from Bailing production bacterium Cordyceps Chinese Hirsutella for synthesizing metabolic (desoxy) pyrimidine nucleoside triphosphate from (desoxy) pyrimidine nucleoside diphosphate, a gene for coding the enzyme and application thereof. The enzyme is nucleoside diphosphokinase which has more than 90% of homology with amino acid sequence disclosed as SEQ ID NO.1; and the coding gene has more than 90% of homology with nucleotide sequence disclosed as SEQ ID NO.2. The invention researches the metabolic pathway of (desoxy) pyrimidine nucleoside diphosphate synthesized (desoxy) pyrimidine nucleoside triphosphate in details in principle. The cloned DNA (deoxyribonucleic acid) comprising the nucleotide sequence provided by the invention can be transformed into engineering bacterium by transduction, conversion and conjugal transfer. By adjusting the expression of the (desoxy) pyrimidine nucleoside triphosphate biosynthesized gene, the host (desoxy) pyrimidine nucleoside triphosphate is endowed with high expressivity, thereby providing an effective way for enhancing the yield of the (desoxy) pyrimidine nucleoside triphosphate and having great application prospects.

The invention relates to a method for preparing 2-C-methyl-D-ribotide-1,4-lactone, which comprises the following steps: adding a raw material D-glucose into dibenzyl amine, acetic acid and ethanol at room temperature, dissolving by stirring, heating, and refluxing to generate 1-desoxy-1-(N,N-amino)-D-fructose; after finishing the reaction, cooling to room temperature to obtain a white solid, drying to obtain 1-desoxy-1-(N,N-amino)-D-fructose, dissolving the 1-desoxy-1-(N,N-amino)-D-fructose and CaO in ethanol and water by stirring, and heating under reflux; and after finishing the reaction, cooling, carrying out centrifugal drying to remove the solvent, adding water and oxalic acid hydrate to precipitate abundant calcium oxalate, filtering, washing, carrying out centrifugal drying on the filtrate to obtain a black viscous liquid, adding acetone, cooling by standing, and recrystallizing with acetone to obtain the 2-C-methyl-D-ribotide-1,4-lactone. The method has the advantages of reasonable technique, low cost, short reaction time and high yield, and is simple to operate.

The invention discloses a synthesis method of 9-desoxy-9-homoerythromycin A(Z) oxime, which comprises the following steps: adding 9-desoxy-9-homoerythromycin A(E) oxime into an organic solvent, wherein the mass-volume ratio of the 9-desoxy-9-homoerythromycin A(E) oxime to the organic solvent is 1g:(3-10)ml; stirring until the 9-desoxy-9-homoerythromycin A(E) oxime is completely dissolved, and adding an alkali, wherein the mole ratio of the 9-desoxy-9-homoerythromycin A(E) oxime to the alkali is 1:(0.2-1.0); stirring at 0-5 DEG C for 64-82 hours; and after the reaction finishes, filtering, washing the obtained filter residue with a 0-5-DEG C organic solvent to obtain a white solid, and carrying out vacuum drying on the white solid to obtain the 9-desoxy-9-homoerythromycin A(Z) oxime finished product. The method is very simple in technical process and very convenient to operate. The synthesized 9-desoxy-9-homoerythromycin A(Z) oxime has the advantages of high purity, no color change and high yield.

The invention relates to a method for preparing 2-C-methyl-D-ribotide-1,4-lactone, which comprises the following steps: adding a raw material D-glucose into dibenzyl amine, acetic acid and ethanol at room temperature, dissolving by stirring, heating, and refluxing to generate 1-desoxy-1-(N,N-amino)-D-fructose; after finishing the reaction, cooling to room temperature to obtain a white solid, drying to obtain 1-desoxy-1-(N,N-amino)-D-fructose, dissolving the 1-desoxy-1-(N,N-amino)-D-fructose and CaO in ethanol and water by stirring, and heating under reflux; and after finishing the reaction, cooling, carrying out centrifugal drying to remove the solvent, adding water and oxalic acid hydrate to precipitate abundant calcium oxalate, filtering, washing, carrying out centrifugal drying on the filtrate to obtain a black viscous liquid, adding acetone, cooling by standing, and recrystallizing with acetone to obtain the 2-C-methyl-D-ribotide-1,4-lactone. The method has the advantages of reasonable technique, low cost, short reaction time and high yield, and is simple to operate.

The invention discloses a specificity monoclonal antibody capable of distinguishing various carbadox and cyadox metabolism products and an enzyme linked immunosorbent assay method and kit for detecting the carbadox and cyadox metabolism products. According to the invention, the monoclonal antibody is secreted by a hybridoma cell strain DCBX5B1 of which the preservation number is CCTCC NO: C201495. Compared with the prior art, the monoclonal antibody disclosed by the invention can distinguish DCBX, bisdesoxy cyadox and desoxy cyadox (N4) at the same time, and has higher sensitivity and specificity. The ELISA method and the kit, disclosed by the invention, can detect the residue of the carbadox and cyadox metabolism products in meat food at the same time, and have the advantages of high detection efficiency, high sensitivity, high precision, high accuracy and the like.

The present invention relates to a novel podophyllotoxin derivatives. Its anti-tumor activity is raised and its loxicity is reduced. Said invention also provides its structural formula.

The invention belongs to the technical field of chemical medicines, and particularly relates to a Beta-L-2'-desoxy-thymine nucleoside derivative, a preparation method and purposes thereof. The Beta-L-2'-desoxy-thymine nucleoside derivative has a structure as showed in a format I, wherein R1 and R2 are independent O, S or Se; when one of the R1 and the R2 is O, R3 is halogen, -OH, -NH2, C1-C8 alkyl, (CH2)nF, (CH2)n-1CHF or CF3; R4 is halogen, H, or CF3; and n is 1-8. The invention provides the derivative which has activity of resisting hepatitis virus, and offers a new choice for preparing medicines capable of treating the hepatitis.

This invention discloses 3-desoxy-2-methylene-19-nor-vitamin D analogs, and specifically (20S)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 and (20R)-3-desoxy-2-methylene-1α,25-dihydroxy-19-nor-vitamin D3 as well as pharmaceutical uses therefor. These compounds exhibit relatively high binding activity and pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to monocytes thus evidencing use as anti-cancer agents especially for the treatment or prevention of osteosarcoma, leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. These compounds also exhibit relatively high calcemic activity evidencing use in the treatment of bone diseases.