15 results about "Site selectivity" patented technology

The application provides a simple and efficient synthesis method, and realizes the method for generating a seven-membered phosphine oxide compound by C-P bond activation insertion of an alkyne of a five-membered phosphine oxide compound through a phosphine oxygen ligand connected nickel-aluminum bimetallic catalyst, and belongs to the technical field of method development. The key to solving the problem of the application lies in that: 1. A five-membered phosphine oxide compound which is efficient and specific in reaction activity and site selectivity is found, and a method for realizing C-P bond activation by means of a tension ring is found; 2. A bimetallic catalytic system is designed by using the characteristics of the phosphine oxygen ligand, so that the reaction activity is greatly improved, and therefore the preparation is more efficient.

The present application relates to the technical field of pharmaceutical chemistry, and particularly relates to a fluorinated camptothecin drug derivative, a preparation method and application thereof. The present application provides a preparation method of a fluorinated camptothecin drug derivative, comprising the following steps: dispersing a camptothecin drug derivative as shown in formula (II) and a fluorination reagent in a solvent, carrying out a reaction at room temperature, and separating and purifying a reaction mixture obtained after the reaction, so as to obtain the fluorinated camptothecin drug derivative as shown in formula (I); the fluorinated camptothecin drug derivative in the present application is prepared by directly fluorinating the camptothecin drug derivative, the operation process is simple, the reaction condition is mild, the site selectivity is high, the reaction is efficient, and the fluorinated camptothecin drug derivative can be prepared by only one step reaction. In addition, the fluorinated camptothecin drug derivative in the present application has good antitumor activity, and provides a new scheme for antitumor drugs.

The invention relates to the technical field of benzene selenate compound ortho-position selective C-H bond boronation, in particular to a lewis acid promoted benzene selenate compound ortho-position selective C-H bond boronation method which comprises the following steps: under the action of lewis acid, benzene selenate shown in a formula (I) and boron trihalide are subjected to a C-H bond boronation reaction, and the benzene selenate compound shown in the formula (II) is obtained. Preparing a compound as shown in a formula (II) under the protection of pinacol; wherein R is independently selected from any one of hydrogen, C1-C6 alkyl, halogen and C6-C14 aryl. Cheap lewis acid is used for promoting, through coordination of boron trihalide and carbonyl in the benzene selenate compound, the benzene selenate compound is subjected to a C-H bond boronation reaction, then under protection of pinacol, a series of benzene selenate borate compounds are obtained, and the method is high in site selectivity and low in cost.

The application belongs to the technical field of chemical industry and relates to a preparation method of a novel chiral bipyridine and application of the chiral bipyridine in catalytic reaction. Various benzyl bromides with 4,5-diazofluorene as a skeleton are reacted to generate a series of chiral bipyridine ligands, then under the participation of the ligands, indolines and quinoline nitrogen-containing heterocyclic compounds are reacted with pinacol diboronic acid under the catalysis of [IrOMe(COD)2] as a metal catalyst, and then a series of phenol compounds are obtained through oxidation of sodium perborate. The novel chiral bipyridine ligand developed by the method has the advantages of good site selectivity and excellent reaction yield without using strong acid and strong base in the process of C-H bond selective boronation.

The application provides a kind of containing spiro compound and its preparation method and application, belong to organic synthesis technical field.The structure formula of containing spiro compound described in the application is as shown in formula 1, formula 2 or formula 3: formula 1, formula 2, formula 3, in formula 1, formula 2 and formula 3, R2It is selected from hydrogen, deuterium, methyl, methoxy, hydroxyl or halogen, R3It is selected from hydrogen, methyl, halogen, cyano or trifluoromethyl, R4It is selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted benzyl, substituted or unsubstituted phenyl, cyclic alkyl containing double bond or deuterated methyl, R5It is selected from substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted naphthyl, unsubstituted phenyl or phenyl substituted by one or more of halogen, methyl, tert-butyl, methoxy, alkyl, n is the positive integer of 0-3.The application realizes excellent site selectivity, avoids C3 position side reaction, and has good chemical selectivity.

The application provides a simple and efficient synthesis method for synthesizing a novel binaphthol derivative skeleton phosphorus oxygen ligand, and realizes a method for realizing the enantioselective nickel catalytic aliphatic C(sp 3 )‑H activation of formamide by using a binaphthol derivative phosphorus oxygen ligand connected nickel-aluminum bimetallic catalyst, and belongs to the technical field of asymmetric catalysis application. The key to solving the problem of the application lies in that: 1. A novel binaphthol derivative phosphorus oxygen ligand which is efficient and specific in reaction activity, site selectivity and corresponding selectivity is found, and a method for nickel catalytic aliphatic C(sp 3 )‑H asymmetric activation of formamide is realized; 2. A bimetallic catalyst system is designed by using the characteristics of the ligand, so that the reaction activity is greatly improved, and the efficient preparation is more easy.

The present application relates to a kind of preparation method of triphosphoryl uridine trisodium and its preparation.The present application uses ionic liquid as reaction solvent, 2-chloro-4H-1,3,2-benzene dioxaphosphorin-4-ketone (compound 1) is reacted with tributylammonium pyrophosphate to generate cyclic intermediate 2, then uridine is reacted, and then it is obtained by oxidation, basic hydrolysis ring-opening step triphosphoryl uridine trisodium.The present application uses ionic liquid as solvent to promote the site selectivity of the hydroxyl group in the ribose structure of uridine in the reaction, which can make the reaction intermediate 2 react with the hydroxyl group of the 5' position of uridine with high selectivity, so as to obtain UTP with high yield, and the present application also prepares UTP into the form of trisodium salt to facilitate purification and preservation.The present application solves the problems of long steps and low yield in the prior art when using chemical synthesis method to synthesize UTP.

The invention discloses a method for synthesizing a site-selective diaryl sulfone compound, which comprises the following steps of: orderly mixing sodium sulfinate, biaryl lambda 3 bromine salt / chlorine salt, alkali or catalyst and solvent, and stirring at 0 DEG C or 95 DEG C to construct a C-S bond, so that site selectivity control can be realized by adjusting reaction conditions, and the site selectivity of the diaryl sulfone compound is improved. The diversified synthesis of the diaryl sulfone compound is realized. According to the present invention, the synthesis of the diaryl sulfone compound can be efficiently and selectively achieved at the high site, the used starting raw material has characteristics of simple synthesis, diverse structures and low price, the reaction cost is reduced, the post-treatment step of the reaction is simplified, and the construction of the site-selective C-S bond can be achieved. The synthesis reaction operation is simple, the condition is mild, the yield is high, the post-treatment is convenient, the amplification of the reaction and the subsequent conversion of the product can be realized, and the method has wide application prospect and practical value.

The present application relates to the technical field of synthetic biology, in particular to a novel taxane acetyl hydrolase, nucleic acid molecule, biological material and application thereof. The acetyl hydrolase comprises at least one of the following sequences: the amino acid sequence of the enzyme shown in SEQ ID NO. 1, SEQ ID NO. 9, SEQ ID NO. 16, SEQ ID NO. 19, SEQ ID NO. 21, SEQ ID NO. 24 or a protein with the same function obtained by substitution and / or deletion and / or addition. The above-mentioned biological enzyme has stronger site selectivity and more controllable product spectrum, has clear regional selectivity for taxane acetyl hydrolysis, can reduce excessive hydrolysis and by-products caused by chemical hydrolysis or non-specific esterase, and has important value for green manufacturing application of taxane.

The invention discloses a stable Cu3 cluster catalytic material and application thereof in C (sp3) H and C (sp2) H bond functionalization reaction, and belongs to the crossing field of coordination chemistry and nano materials. According to the copper cluster enantiomer, 4, 5-diphenyl-1, 3-bis (pyridine-2-yl methyl)-4, 5-dihydro-1H-imidazole-3-ammonium chloride is used as a protective ligand, the copper cluster enantiomer is synthesized through a simple one-pot method, and the yield is high. The chemical formula of the cluster is C91H87Cu3F18N17P3, abbreviated as Cu3NC (NHC), the cluster belongs to a triclinic system, the space group is P-1, a is equal to 14.8470 (1), b is equal to 16.7001 (2), c is equal to 19.3691 (2), alpha is equal to 91.311 (1) degrees, beta is equal to 94.283 (1) degrees, gamma is equal to 96.504 (1) degrees, and V is equal to 4755.88 (8) 3. The catalyst utilizes the advantage of dynamic coordination to realize efficient and high-selectivity catalysis of C (sp3) H and C (sp2) H bond functionalization reaction, has the advantages of excellent chemical selectivity (up to 100%), site selectivity (up to 100%), high efficiency (conversion number (TON) = 123200), high yield (up to 99%), wide substrate range (45), mild condition (room temperature) and the like, and realizes the application and development of the functionalized cluster catalyst.

The invention provides a simple and efficient synthesis method, in particular to a method for realizing insertion of a formyl compound C-H into intramolecular olefin to construct an indolone compound containing a chiral quaternary carbon center by connecting a phosphorus-oxygen ligand with a nickel-aluminum bimetallic catalyst, and belongs to the technical field of methodology development. The key of the problem solved by the invention is as follows: 1, a formyl compound which is efficient and specific in reaction activity and site selectivity is found; 2, a bimetallic catalytic system is designed by utilizing the characteristics of phosphine oxide ligands, so that the reaction enantioselectivity is greatly improved;

The invention discloses a preparation method of famciclovir. The preparation method comprises the following steps: reacting diethyl malonate serving as a starting material with ethylene oxide to obtain an intermediate 1, reacting the intermediate 1 with paratoluensulfonyl chloride to generate an active ester side chain intermediate 2, and performing high-selectivity substitution reaction on the active ester side chain intermediate 2 and the ninth site of 2-amino-6-chloropurine to obtain a key intermediate 3; the intermediate 3 is subjected to ester bond reduction and ester formation through an existing mature famciclovir process, and finally pd / C dechlorination is performed to obtain the famciclovir. Compared with methods reported in existing literatures, the method has the advantages that raw materials are simple and easy to obtain, reaction conditions are simple, 9-site selectivity is larger than 99%, the total reaction yield is high, and industrial large-scale production is facilitated.

The application discloses a method for preparing branched polypeptides based on chemical-enzyme step-by-step functionalization, and belongs to the field of cross between biotechnology and synthetic chemistry. The method uses a peptide A containing an asparagine residue at a C terminal and a peptide B containing a cysteine residue at an N terminal as raw materials, first uses polypeptide amidase PAM15 to catalyze the reaction of the peptide A and hydrazine to generate a diacylhydrazine intermediate; then the diacylhydrazine intermediate is subjected to azidation by low-temperature sodium nitrite to obtain a diacyl azide intermediate; finally, the diacyl azide intermediate is selectively connected with the peptide B to obtain a branched polypeptide with an asparagine as a core branched node. The application has high site selectivity, requires less amount of a protecting group, has strong sequence compatibility, and has a clear product structure, breaks through the limitation of traditional lysine nodes, can efficiently construct diversified branched polypeptides, and is suitable for fields such as biomaterials, antibacterial peptides and vaccine research and development.

The invention discloses a method for coupling polypeptide or protein and oligonucleotide promoted by visible light, which comprises the following steps: taking polypeptide or protein at least containing one free and solvent-exposed cysteine as a raw material, and oligonucleotide or 6-aza-uracil derivative containing 6-aza-uracil nucleoside as another raw material; a pyridinium salt is used as an activating reagent, a buffer solution is used as a reaction solvent, and polypeptide or protein and oligonucleotide are coupled to form a stereoscopically retained stable C-C bond under the participation of an additive and the irradiation of visible light. The configuration of the conjugate obtained by the invention at a modification site is maintained. Meanwhile, the method has excellent site selectivity, accurate modification of polypeptide or protein can be realized, the reaction is carried out under a biocompatible condition, a catalyst or a reducing agent does not need to be added, the reaction efficiency is high, biocompatibility is realized, and disulfide bonds in the polypeptide or the protein can be compatible.

The invention provides an MLM type structure triglyceride rich in DHA (docosahexaenoic acid) at sn-2 site as well as a preparation method and application of the MLM type structure triglyceride. The triglyceride has a glycerin skeleton, the sn-2 site of the glycerin skeleton is esterified with DHA, the sn-1 site and the sn-3 site of the glycerin skeleton are independently esterified with one of C6-C12 saturated medium-chain fatty acids, and at least one of the sn-1 site and the sn-3 site is esterified with lauric acid. The DHA is fixed at the sn-2 position, and lauric acid is introduced at the sn-1 and sn-3 positions, so that the effects of improving the DHA enrichment degree of the colon and cooperatively inhibiting the colorectal cancer are achieved. The triglyceride with the structure belongs to a typical lipid with a middle-long-middle (MLM) type structure. According to the molecular design, DHA is reserved in a monoacylglycerol form in the digestion process and acts on the colon in a positioned manner by utilizing the characteristic that digestive enzyme is selective to a triglyceride part, and meanwhile, lauric acid is rapidly absorbed to play an anti-tumor immunoregulation role, so that complementary advantages of two functional fatty acids are realized on the molecular level.