专利号:US-11512303-B2 优先权日:2017-05-27 标 题 :Engineered polypeptides and their applications in the synthesis of beta-hydroxy-alpha-amino acids 发明人:CHEN HAIBIN; BONG YONG KOY; XU QING; ZHOU AMENG; SHEN TIANRAN; YANG JIADONG; YANG ZHUHONG 权利人:ENZYMASTER NINGBO BIO ENG CO LTD 摘要:The present invention provides engineered polypeptides that are useful for the asymmetric synthesis of β-hydroxy-α-amino acids under industrial-relevant conditions. The engineered polypeptides disclosed in this invention were developed through directed evolution based on the ability of catalytic synthesis of (2S, 3R)-2-amino-3-hydroxy-3-(4-nitrophenyl) propanoic acid. The present disclosure also provides polynucleotides encoding engineered polypeptides, host cells capable of expressing engineered polypeptides, and methods of producing β-hydroxy-α-amino acids using engineered polypeptides. Compared to other processes of preparation, the use of the engineered polypeptides of the present invention for the preparation of β-hydroxy-α-amino acids results in high purity of the desired stereoisomers, mild reaction conditions, low pollution and low energy consumption. So, it has good industrial application prospects.
专利号:US-11078465-B2 优先权日:2018-02-12 标题:Alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols 发明人:NI YE; WANG YUE; DAI WEI; XU GUOCHAO; ZHOU JIEYU 权利人:UNIV JIANGNAN 摘要:The present disclosure discloses an alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols, and belongs to the technical field of bioengineering. The alcohol dehydrogenase mutant of the present disclosure has excellent catalytic activity and stereoselectivity, and may efficiently catalyze the preparation of a series of chiral diaryl alcohols in R- and S-configurations. By coupling alcohol dehydrogenase of the present disclosure to glucose dehydrogenase or formate dehydrogenase, the synthesis of chiral diaryl alcohol intermediates of various antihistamines may be achieved. Compared with the prior art, a method for preparing diaryl chiral alcohols through asymmetric catalytic reduction using the alcohol dehydrogenase of the present disclosure has the advantages of simple and convenient operation, high substrate concentration, complete reaction and high product purity, and has great industrial application prospects.
专利号:US-10487099-B2 优先权日:2017-06-30 标 题:Synthesis of hypervalent iodine reagents with dioxygen 发明人:POWERS DAVID CHARLES; MAITY ASIM; HYUN SUNG-MIN 权利人:TEXAS A & M UNIV SYS 摘要:Methods of synthesis of hypervalent iodine reagents and methods for oxidation of organic compounds are disclosed.
专利号:US-6620942-B2 优先权日:1998-12-23 标题 :Synthesis of histamine dihydrochloride 发明人:YEH WEN-LUNG; ANTCZAK CASIMIR; MCGOLRICK JEFFRY DAVID; ROTH MICHAEL JOSEPH; WRONA MARK 权利人:MAXIM PHARMACEUTICALS 摘要:The invention disclosed herein relates to the preparation of pharmaceutical grades of histamine dihydrochloride using a two step non-enzymatic synthetic method. The invention disclosed herein describes the synthesis of histamine dihydrochloride by the non-enzymatic decarboxylation of histidine and the step-wise conversion of the decarboxylated product to the dihydrochloride salt form. The invention disclosed herein considers a final product of histamine dihydrochloride containing less than each of the following: 0.8% L -histidine HCl monohydrate, 0.1% individual chromatographic impurities, and 2% total impurities, to be acceptable for pharmaceutical use.
专利号:US-2022098155-A1 优先权日:2018-11-14 标 题 :Novel pathway for the synthesis of diazirines, that may or may not be enriched in nitrogen-15 发明人:REBOUL VINCENT; FRANCK XAVIER; GLACHET THOMAS; MARZAG HAMID 权利人:UNIV ROUEN NORMANDIE; UNIV CAEN; INSTITUT NAT DES SCIENCES APPLIQUEES DE ROUEN INSA; CENTRE NAT RECH SCIENT; ECOLE NAT SUPERIEURE DINGENIEURS DE CAEN 摘要:The present invention concerns a novel method for synthesising diazirines, that may or may not be enriched in nitro-gen-15, from amino acids or imines, via a one-pot synthesis method, comprising the reaction of the starting amino acid or imine with ammonia, which may or may not be enriched in nitrogen-15, and a hypervalent iodine oxidant. The present invention also relates to a method for synthesising ammonia enriched in nitrogen-15. The invention also concerns certain diazirines of formula (I) likely to be obtained by the claimed synthesis method, and also refers to the 15 N 2 -diazirines of formula (I′). The claimed diazirines can be used in photoaffinity labelling. The 15 N 2 -diazirines can also be used in hyperpolarisation, in particular in the medical imaging field.
专利号:US-2022356182-A1 优先权日:2009-03-27 标题 :Inhibitors of hepatitis c virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.