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117results about How to "Stereoselective" patented technology

Synthesis process of vecuronium bromide

The invention discloses a synthesis process of vecuronium bromide. The synthesis process comprises the following steps: generating epiandrosterone sulfonyl ester (III) by carrying out esterification reaction between epiandrosterone (II) and paratoluensulfonylchloride; generating 5Alpha-androst-2-alkene-17-ketone (IV) by carrying out elimination and dehydration reaction between the (III) and 2,6-lutidines; generating 17-acetoxyl-5Alpha-androstane-2,16-diene (V) by carrying out enolization and esterification reaction between the (IV) and isopropenyl acetate; generating (2Alpha, 3Alpha, 16Alpha,17Alpha)-diepoxy-17Beta-acetyl-5Alpha-androstane (VI) by epoxy reaction of the (V) under the effect of hydrogen peroxide; generating 2Beta, 16Beta-di(1-piperidyl)-5Alpha-androstane-3Alpha-hydroxyl-17-ketone (VII) by ring-opening and addition reaction of the (VI) under the effect of hexahydropyridine; generating 2Beta, 16Beta-di(1-piperidyl)-5Alpha-androstane-3Alpha,17Beta-diol (VIII) by the (VII)under the reduction of potassium borohydride; generating 2Beta, 16Beta-di(1-piperidyl)-3Alpha, 17Beta- acetoxyl-5Alpha-androstane (IX) by carrying out esterification reaction of the (VIII) under the acetylation of acetic anhydride; and generating vecuronium bromide (I) by carrying out quaternary ammonium salt reaction between the (IX) and bromomethane. The invention has the advantages of low cost,less pollution and high yield.
Owner:XUZHOU NORMAL UNIVERSITY

Immobilized recombinant penicillin G acylase and application thereof

The invention discloses an immobilized recombinant penicillin G acylase and an application thereof to preparation of (S)-2-aryl-amino acid and cephalosporin antibiotics. The immobilized recombinant penicillin G acylase disclosed by the invention is capable of converting an S-type substrate into an S-type product within shorter time, high in substrate tolerance and strict in S selectivity for the substrate and structural analogues thereof; due to the addition of cobalt ions as well as a protective agent with phenylacetic acid and glycerin as enzyme active centers, the immobilized recombinant penicillin G acylase disclosed by the invention is prevented from being successfully subjected to multipoint covalent immobilization on the surface of an epoxy resin carrier under the condition that enzyme molecules are seriously inactivated in an immobilization process, and the immobilization method is simple and feasible, cheap in raw materials and suitable for large-scale operation; the immobilized recombinant penicillin G acylase can be used for synthesizing cephalosporin antibiotics and splitting the prepared (S)-2-aryl-amino acid, and can be continuously used for more than 50 batches before the activity of the immobilized enzyme is not remarkably reduced.
Owner:ZHEJIANG UNIV OF TECH

Preparation method of methyl (R)-o-chloromandelate utilizing biocatalytic asymmetric reduction

The present invention discloses a preparation method of methyl (R)-o-chloromandelate utilizing biocatalytic asymmetric reduction and used recombinant vectors and genetically engineered bacteria. The preparation method comprises the step of carrying out biotransformation reaction on methyl o-chlorobenzoylformate used as the substrate with genetically engineered bacteria wet cells or freeze-dried cells capable of coexpressing recombinant reductase and recombinant glucose dehydrogenase as the catalyst at pH 6-8 in the presence of glucose, wherein the recombinant reductase is a recombinant aldo-keto reductase. The genetically engineered bacteria whole cells can simultaneously express the aldo-keto reductase and glucose dehydrogenase and can achieve high-efficiency regeneration of intracellular coenzyme NADP<+>. By using the preparation method, high-concentrations methyl o-chlorobenzoylformate can be catalyzed and completely transformed into methyl (R)-o-chloromandelate with a single conformation, without adding a coenzyme. Because of expensive coenzyme, the preparation method provided by the invention greatly lowers the production cost, has mild reaction conditions, is environmentally-friendly and simple to operate, and has good industrial application prospects.
Owner:EAST CHINA UNIV OF SCI & TECH

Amino-acid ester derivative cation type chiral ionic liquid and preparation method thereof

The invention provides an amino-acid ester derivative cation type chiral ionic liquid and a preparation method thereof. A general formula of the amino-acid ester derivative cation type chiral ionic liquid is A<+>X<->, wherein A<+> represents an amino-acid ester cation derivative, and X<-> represents one of BF4<->, PF6<-> and HSO4<->. The preparation method comprises steps as follows: amino acid, methyl alcohol and thionyl chloride react at the low temperature, and amino acid ester hydrochloride is obtained; amino acid ester hydrochloride has a Mannich reaction with paraformaldehyde and acetone, and amino acid ester derivative Mannich base is obtained; amino acid ester derivative Mannich base reacts with bromo-hydrocarbon, and a bromate type chiral ionic liquid of the amino-acid ester derivative is obtained; bromide ions of the bromate type chiral ionic liquid of the amino-acid ester derivative are exchanged, and the amino-acid ester derivative cation type chiral ionic liquid is obtained. The amino-acid ester derivative cation type chiral ionic liquid has the multiple advantages of high selectivity of a chiral substance as well as non-volatility, non-toxicity and pollution prevention of an ionic liquid, and is suitable for large-scale production of the fine chemical industry.
Owner:TANGSHAN NORMAL UNIV
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