133 results about "Compound E" patented technology

Composition for post-treating anodized aluminum and aluminum alloys and the process for using said composition to improve the corrosion-resistance, abrasion, and adhesion bonding properties of the anodized aluminum and its alloys. The composition comprises an acidic aqueous solution having a pH ranging from about 2.5 to 4.5 containing effective amounts of trivalent chromium salts, alkali metal hexafluorozirconates, an alkali metal fluoro-compound e.g. fluoroborates and/or fluorosilicates, and effective amounts of water soluble thickeners and surfactants.

Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.

The invention discloses an Apixaban preparation method. The Apixaban preparation method comprises that 1, an intermediate I and an intermediate II undergo a [3+2] cyclization addition reaction under the alkali action to produce a compound B, and the compound B undergoes a morpholine ring removal reaction under the acid condition to produce a compound C, 2, the compound C is reduced by iron powder to form a corresponding amino compound D, 3, the amino compound D and 5-chlorovaleryl chloride undergo an amidation reaction under the triethylamine action to produce a compound E, 4, the compound E undergoes a cyclization reaction under the strong base action to produce a compound F, 5, the compound F undergoes a hydrolysis reaction under the strong base action to produce a corresponding carboxyl compound G, and 6, the carboxyl compound G and CDI undergo a reaction to produce an active intermediate H and the active intermediate H and ammonia water undergo an aminolysis reaction to produce the desired compound A. The Apixaban preparation method has simple processes, does not need strict reaction conditions, has low equipment requirements, has high reaction yield, utilizes stable intermediates thereby solving intermediate storage problems, and effectively improves product purity.

The invention relates to a method for preparing compound palbociclib (shown as the formula I). A compound D (shown as the formula II) serves as a raw material, and a compound E (shown as the formula III) is obtained through a rearrangement reaction of alkenyl ether; then the compound E is subjected to t-butyloxycarboryl protection group removal under the acidic condition, and target product palbociclib is obtained; an R group in a compound D is selected from any one of a C1-C6 alkyl group, a C1-C6 halogenate alkyl group, C1-C6 hydroxyalkyl and a C1-C6 naphthenic base. The process procedure and operation steps are easy and convenient, prepared palbociclib is high in purity, and good popularization prospects are achieved.

The present invention relates to the effect of naturally occurring compounds on tumor development. As an example of proof, we used low; non-toxic doses of three compound e.g. Calcium D-glucarate, a naturally occurring Ca⁺⁺ salt of D-glucaric acid; Nicotinamide (NA), a naturally occurring vitamin and butyric acid (BA), a naturally occurring saturated short chain fatty acid. 7,12 dimethylbenzanthracene (DMBA), which is a very potent skin carcinogen and is an environmental pollutant, was used for skin tumor development. Experiment was performed upto 30 weeks. All the above-mentioned compounds were used either alone or concomitantly any two or all the three. In the positive control group 100% tumorigenesis was attained in 28 weeks, use of single compound led to the inhibition of DMBA induced tumorigenesis between 33 to 47%, use of two compounds resulted in the 73 to 80% reduction in tumorigenesis but the concomitant use of three compounds resulted into 100% inhibition of tumor development at the end of 30 weeks. This led us to conclude that the concomitant use of Cag, NA and BA in combination of two is useful for preventing skin tumor develoment for a sort or long period of time. But the concomitant use of all the three compounds, as described, exhibited the perfect synergistic effect in preventing the tumor development completely. This strategy should be equally effective in the management of benign and possibly malignant tumor in any organ caused by any mean.

The present invention relates to the method of treatment or prophylaxis of patients with drug-induced liver diseases which comprises administering to the patient in need thereof a therapeutically effective amount of a mitochondrially targeted antioxidant compound e.g. derivatives of vitamin E, coenzyme Q₁₀ or a glutathione peroxidase mimetic. The present invention also relates to pharmaceutical compositions containing the antioxidant(s) intended for such use.

The invention discloses a dihydropyrimidine compound as well as a preparation method and an application thereof, and belongs to the technical field of medicinal chemistry. The structure of the dihydropyrimidine compound provided by the invention is as shown in a formula I in the specification. The preparation method provided by the invention comprises the following steps: carrying out substitution reaction on a compound a and a compound k under the catalysis of alkali to generate a compound b; performing substitution reaction on the compound c and the compound d under an alkaline condition to obtain a compound e; carrying out Mitsunobu reaction on the compound e and f to obtain an intermediate g, and carrying out coupling reaction on the compound g and b to generate a compound h. The invention provides the application of the compound shown in the formula I or salt, solvate, allomer, metabolite, nitric oxide and prodrug thereof in preparation of drugs for treating or preventing P2X3 and/or/P2X2/3 receptor related diseases. The dihydropyrimidine compound disclosed by the invention has a good P2X3 receptor antagonism effect and better safety.

The invention discloses E-configuration benzamide compounds, and a pharmaceutical preparation application thereof. The structure of the E-configuration benzamide compounds is disclosed as Formula (I); the chemical name is N-(2-amino-4-fluorophenyl)-4-[N-[(E)-3-(3-pyridyl)acryloyl]aminomethyl]benzamide; and in the structural formula, the configuration of the 3-pyridylacryloyl group is E. The E-configuration benzamide compounds disclosed as Formula (I) have subtype selective histone deacetylase inhibition activity, and are mainly used for inhibiting HDAC1, HDAC2 and HDAC3 in Class I HDAC and HDAC10 in Class IIb HDAC. The E-configuration benzamide compounds disclosed as Formula (I) can be used for treating diseases related to histone deacetylase activity abnormity, such as cancers, including lymphomata, entity tumor, blood system tumors and the like.

Two-component adhesives (K), which includes two components K1 and K2. Component K1 includes at least one epoxy resin A with more than one epoxy group per molecule on average; at least one epoxy adduct B with more than one epoxy group per molecule on average that is an epoxy adduct of type B1 and optionally combined with an epoxy adduct of type B2; at least one reaction product F between an epoxy adduct B and a compound C, which has at least two isocyanate groups, in addition to at least one curing agent D for epoxy resins, which is activated by increased temperature. The component K2 comprises a compound E, which includes at least two isocyanate groups.

The invention discloses a method for preparing a halofuginone intermediate shown in a formula D or E. The method comprises the following steps of: (1) dropwise adding solution of a compound F into benzyl chloroformate solution, and performing Van Braun reaction to obtain a compound E; and (2) performing Claisen rearrangement reaction on the compound E obtained in the step (1). By the method, the Van Braun reaction can be completely performed, the using amount of benzyl chloroformate is reduced, the efficiency of the reaction is improved, and a 2-bit product can be selectively obtained in the subsequent Claisen rearrangement reaction. In the better embodiment of the invention, the operation process is simplified by a one-pot method, the using amount of solvents is reduced, the selectivity is improved, the cost of the reaction is reduced, the pollution to the environment is reduced, and good conditions are created for mass production of halofuginone.

The invention relates to a bone peptide composition, which comprises the following components in part by weight: 8 to 10 parts of bond polypeptide compound A, 5 to 8 parts of bone polypeptide compound B, 5 to 8 parts of bone polypeptide compound C, 4.5 to 7.5 parts of bone polypeptide compound D, 3 to 6 parts of bone polypeptide compound E, 16 to 22 parts of free amino acid, 0.3 to 5.4 parts of ribose, 0.04 to 0.12 parts of trace element and 0 to 0.01 parts of free fatty acid, wherein amino acid sequences of the bone polypeptide compounds A, B, C, D and E are measured. The invention also relates to a preparation method and application of the bone peptide composition. The preparation method is simple, convenient, easy to operate and high in yield, and the prepared bone peptide composition is high in bioactivity.

The invention discloses polyester and a production method thereof. The polyester at least contains a compound A derived from an inorganic antimony compound, a compound B derived from an organic acid calcium compound, a compound C derived from an organic acid lithium compound, a compound D derived from a stabilizer organic phosphorus compound and a compound E derived from inorganic phosphate, wherein the content of phosphorus elements in the inorganic phosphate relative to the weight of polyester is 1-200ppm. The invention has obvious advantages, an obtained polyester slice has favorable hydrolysis resistance, and a polymer has small foreign matter size.

The invention relates to a production method of low-acetaldehyde titanium system polyester, which is mainly used for solving the problem of relatively large amount of acetaldehyde residue in the polyester prepared by use of a titanium system catalyst before. The technical scheme adopts a catalyst obtained by the reactions of the following raw materials: (1) a titanium compound A:Ti(OR)4 with the general formula shown in the specification, wherein R is straight-chain or branched alkyl with 1-10 carbon atoms; (2) diol B with 2-10 carbon atoms; (3) a metal compound C selected from the periodic table of elements IA; (4) at least one aliphatic organic acid D selected from organic acids; (5) at least one phosphate compound E selected from phosphorus compounds; and (6) at least one metal compound F selected from IIA, IB, IIB, VIIB and VIII of the periodic table of elements. The technical scheme can be used for solving the problem relatively well and can be applied to industrial production of polyester with low acetaldehyde residue.

The invention discloses a mint tobacco compound e-liquid. The e-liquid is compounded by tobacco extracts, mint type spice and auxiliary spice, by substituting traditional free nicotine with the tobacco extracts, the stimulation feeling and discomfort brought by the traditional free nicotine are avoided, the mint taste e-liquid good in sensory perception is obtained, the cooling feeling of mint canbe tenderly and slowly released, the aroma of cigarette is achieved, the mouthfeel is tender and smooth, and the smoking taste is closer to traditional mint tobacco.

The invention relates to the field of medicine synthesis, and in particular to chenodeoxycholic acid and a preparation method thereof. The preparation method of the chenodeoxycholic acid provided by the invention comprises the following steps of: using 3 alpha,7 alpha-dihydroxy-5 alpha-ursodeoxycholic acid as raw materials to form an intermediate compound E through chemical reaction; then, performing chemical reaction on the intermediate compound E to form the chenodeoxycholic acid. The structure formula of the intermediate compound E is shown in the description, wherein R1 is alkyl, alkenylor aromatic group; R2 is acyl. The preparation method has the advantages that extracted byproducts can be used as raw materials for fast synthesizing the chenodeoxycholic acid; each step in the process is mild in condition; the yield is high; the method is suitable for mass preparation.

The invention relates to a new high-yield preparation method of azoxystrobin. The method adopts a backward two-step etherification reaction to synthesize azoxystrobin, and concretely comprises the following steps: 1, carrying out an etherification reaction on 2-hydroxybenzonitrile (a compound B) and 4,6-dichloropyrimidine (a compound C) in the presence of a catalyst to obtain 4-chloro-6-(2-cyanphenoxyl)-pyrimidine (a compound D); and 2, carrying out an etherification reaction on the compound D and (E)-3-methoxy-2-(2-hydroxyphenyl )-methyl acrylate in the presence of the catalyst to obtain azoxystrobin, wherein the same catalyst is used in the two-step etherification reaction, and is a compound F. The method improves the total yield to 80-85%.

The invention relates to a method for producing a low-acetaldehyde polyester product. The method is mainly used for solving the problem that the residual of acetaldehyde in polyester bottles prepared by a titanium-series catalyst is relatively high. According to the method, through adopting the technical scheme that a catalyst, which is prepared through carrying out a reaction on the following raw materials: (1) a titanium compound A with a general formula as follows: Ti(OR)4, wherein R is selected from C1-10 straight-chain or branched alkyl; (2) diol B with 2 to 10 carbon atoms; (3) a metal compound C selected from IA of the periodic table of elements; (4) at least one aliphatic organic acid D selected from organic acids; (5) at least one phosphate compound E selected from phosphorus compounds; and (6) at least one metal compound F selected from IIA, IB, IIB, VIIB and VIII of the periodic table of elements, is used, the problem is better solved, so that the method can be applied to the industrial production of polyesters with low acetaldehyde residual.

A curable silicone rubber composition is described for an LED enclosure or packaging. A process for preparing the same and the use thereof are also described. Particularly, the compositions can include at least one tackifier component D, which includes:

• • a) a alkenyl or hydrosilyl group including an isocyanurate compound E, and
  • b) an adhesion-imparting ingredient having at least two functional groups selected from the group consisting of alkenyl, epoxy, alkoxy and hydrosilyl groups, which includes of polysiloxane F and optional coupling agents G.

A process for preparing a ketone by conversion of a compound E which contains an epoxy group to the ketone in the presence of a mixture comprising at least one noble metal and at least one metal oxide as a catalyst system, wherein the metal oxide in the catalyst system is at least one of titanium dioxide and zirconium dioxide, and the process is conducted at 0 to 0.9 bar of hydrogen.

The invention relates to the technical field of medicines and relates to a reference compound for controlling quality of fondaparinux sodium. Relevant reference compounds of fondaparinux sodium include a reference compound A (Rrt0.45), a reference compound B (Rrt0.54), a reference compound C (Rrt0.77), a reference compound D (Rrt0.93) and a reference compound E (Rrt1.20).

The invention discloses a synthesis method of a structurally specific salbutamol complete antigen and belongs to the technical field of biochemical engineering. The synthesis method comprises the following steps: dissolving 2-bromo-1-[4-hydroxy-3-(hydroxymethyl)phenyl]aceto-1-ketone in acetone; after adding potassium carbonate, reacting with dibenzylamine to generate a compound B; generating a compound C under catalysis of lithium aluminium hydride; reacting with hydrogen under catalysis of Pd/C to generate a compound D; performing a reductive amination reaction with ethyl levulinate to generate a compound E; and hydrolyzing under alkaline condition, and recrystallizing to generate salbutamol hapten named as 4-((2-hydroxy-2-(4-hydroxy-3-(hydroxymethyl)phenyl)ethyl) amino) valeric acid. A complete antigen is obtained by coupling the carboxyl on the hapten and amidogen on carrier proteins. Experimental results show that the antiserum titer of animals immune to the complete antigen achieves 81,000, the limit of detection is 0.3ng/mL, and half inhibiting concentration is 3.2ng/mL; a generated antibody is high in specificity and sensitivity; the antigen or the antibody has a broad application prospect.

The invention discloses polyimide with a phosphoric acid side chain-containing long chain, a preparation method thereof and application thereof. The polyimide has the structure shown as formula (I). The preparation method comprises the following steps of: dissolving phenolic hydroxyl-containing aromatic diamine monomer and dianhydride in organic solvent A and performing condensation polymerization on the mixture to form a compound a; dissolving the compound a in organic solvent B, and adding a bromination reagent and an alkaline substance into the solution to form a compound b; dissolving the compound b in the organic solvent B, and adding trifluoromethyl methacrylate, trimethylsilyl-terminated hydroxyethyl methacrylate, cuprous chloride, copper chloride and a genin into the solution to form a compound c; dissolving the compound c in the organic solvent B, and dropwise adding acid solution into the solution to form a compound d; dissolving the compound d in the organic solvent B, and adding triethylamine, cuprous chloride and a phosphitylating agent into the solution to form a compound e; and dissolving the compound e in the organic solvent B, and adding trimethyl halogenosilane to perform hydrolysis reaction, and after the hydrolysis reaction, removing the solvent to obtain the polyimide with the phosphoric acid side chain-containing long chain.

The invention discloses a preparing method of lansuola pyrazole, which comprises the following steps: 1) selecting solvent A and water compound solvent B; allocating 2-97% solvent B and 3-98% 2-[3-methyl-4-(2,2,2-trifluoro ethyoxyl)-2-pyridine] sulfide-H-benzimidazole to prepare compound C; 2) blending 0-30% solvent D, 0-80% water and 20-100% oxidant to prepare compound E with the molar rate of oxidant and 2-[3-methyl-4-(2,2,2-trifluoro ethyoxyl)-2-pyridine] sulfide-H-benzimidazole at 0.1-10:1; 3) blending compound C and compound E under -10-50 deg.c; 4) adjusting pH value of composite solution at 5-11 through acid or alkaline; separating to obtain the product.

The present invention relates to a process for the preparation of a polymer P having amide and ester groups in the solid state of aggregation, in a first step (a) a homo- or copolymer P1 of (meth)acrylic acid, itaconic acid or crotonic acid being reacted with at least one monohydroxy compound E at a temperature up to 200° C. to give a polymer P2, so that anhydride groups form in addition to ester groups, in a second step (b) the polymer P2 prepared in step (a) being cooled to below 60° C. so that the polymer P2 is present in the solid state of aggregation or as supercooled melt, and in a third step (c) the polymer P2 having anhydride groups and present in the solid state of aggregation or as supercooled melt being amidated with at least one amine compound A at temperatures below 60° C., the amine compound A used in the third step (c) being present in the solid state of aggregation or on or in a solid carrier material.

The invention provides a synthesis method of toremifene. The synthesis method comprises the following steps: S1. performing McMurry reaction to a compound B as shown in a structural formula II and a compound C as shown in a structural formula III, to obtain a compound D as shown in a structural formula IV; S2. performing selective alkylation reaction of phenolic hydroxyl to the compound D and a compound E as shown in a structural formula V or hydrochloride of the compound E, to obtain a compound F as shown in a structural formula VI; and S3. reacting the compound F with thionyl chloride, to obtain the toremifene, wherein the structural formula II, the structural formula III, the structural formula IV, the structural formula V and the structural formula VI are respectively shown in the specification. The obtained compound D has higher stereoselectivity, therefore, the reaction yield of the toremifene with a Z configuration can be increased when the compound D serves as an intermediate to synthesize the toremifene, and the purity of the toremifene with the Z configuration can be improved; and the synthesis method is stable in technology, mild in reaction conditions, the intermediate is easily separated, and the synthesis method can be used for mass production.