3-苯丙酸乙酯置于硫酸,Sodium Methylate体系中,用 乙醇,硫酸 作为反应溶剂,化学反应 21.5H,反应生成 2-氧代-4-苯基丁酸乙酯 参考文献:Synthesis And Angiotensin Converting Enzyme Inhibitory Activity Of 1,5-Benzothiazepine And 1,5-Benzoxazepine Derivatives. I. 标题:Synthesis And Angiotensin Converting Enzyme Inhibitory Activity Of 1,5-Benzothiazepine And 1,5-Benzoxazepine Derivatives. I. 摘要:新型血管紧张素转化酶(ace)抑制剂的设计与合成,包括(R)-3-氨基-4-氧代-2,3,4,5-四氢-1,5-苯硫氮杂环-5-乙酸(7,26,33 和 37)以及(S)-3-氨基-4-氧代-2,3,4,5-四氢-1,5-苯氧氮杂环-5-乙酸(8 和 27),本文进行了描述.这些系列中的一些化合物在体外和体内显示出强烈的ace抑制活性.同时讨论了结构-活性关系. DOI:10.1248/cpb.34.1128
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-4539150-A 优先权日:1983-06-29 标 题 :Benzothiazepine derivatives and their methods of preparation 发明人:KATAKAMI TSUTOMU; FUKAZAWA NOBUYUKI; IIZUKA HAJIME; NISHINA TAKASHI; SHIRAKAWA ISAO 权利人:MITSUI TOATSU CHEMICALS 摘要:This invention relates to benzothiazepine derivatives of the general formula ##STR1## where K is hydrogen or a --CH 2 COOR 2 group where R 2 is hydrogen or a lower alkyl group, Z is hydrogen or phenyl except when both K and Z are hydrogen, and Y is hydrogen, a --CHR 3 --COOR 1 group, an alkanoyl group or a --COO(CH 2 ) n R 4 group where R 1 is hydrogen or a lower alkyl group, R 3 is hydrogen, an alkyl group, an alkylphenyl group or an aryl-lower alkyl group, R 4 is an aryl group and n is a whole number of 1 to 10, and to their methods of preparation. n The benzothiazepine derivatives of this invention, including their salts, have a powerful inhibitory effect on the angiotensin converting enzyme and exert a marked depressor effect in such models of hypertension as spontaneously occurring hypertensive rats and the like, so that they are useful as drugs for the treatment of hypertension and other cardiovascular diseases. In addition, these compounds are also useful as intermediates for the synthesis of coronary dilators, psychotropic drugs and the like.
专利号:US-5371014-A 优先权日:1988-02-12 标题 :Process for the production of optically active 2-hydroxy acid esters using microbes to reduce the 2-oxo precursor 发明人:MATSUYAMA AKINOBU; NIKAIDO TERUYUKI; KOBAYASHI YOSHINORI 权利人:DAICEL CHEM 摘要:An optically active 2-hydroxy acid derivative is produced by treating a 2-oxo acid derivative with a microorganism, which has been optionally treated, capable of asymmetrically reducing said 2-oxo acid derivative into an optically active (R)- or (S)-2-hydroxy acid derivative represented by the formula (II) and recovering the optically active (R)- or (S)-hydroxy acid derivative thus formed. Optically active 2-hydroxy acid derivatives are important intermediates in the synthesis of various drugs such as a remedy for hypertension.
专利号:WO-2019153634-A1 优先权日:2018-02-12 标题 :Alcohol dehydrogenase mutant and application thereof in synthesis of biaryl chiral alcohol
专利号:HU-P0900712-A2 优先权日:2009-11-13 标题 :New methods and intermediers for the synthesis of ace-inhibitor
[参考文献]: Nai-Dong Shen, Et Al. Efficient Synthesis Of A Chiral Precursor For Angiotensin-Converting Enzyme (Ace) Inhibitors In High Space-Time Yield By A New Reductase Without External Cofactors. Org Lett. 2012 Apr 20;14(8):1982-5. [参考文献]: Ye Ni, Et Al. Scalable Biocatalytic Synthesis Of Optically Pure Ethyl (R)-2-Hydroxy-4-Phenylbutyrate Using A Recombinant E. Coli With High Catalyst Yield. J Biotechnol. 2013 Dec;168(4):493-8.
合成参考文献
摘要:Abou-Hadeed, K.; Hansen, H.-J., Science of Synthesis, (2010) 45, 1063. 摘要:Hari, Y.; Aoyama, T.; Shioiri, T., Science of Synthesis Knowledge Updates, (2010) 4, 30. 摘要:Hari, Y.; Aoyama, T.; Shioiri, T., Science of Synthesis Knowledge Updates, (2010) 4, 27. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 180. 摘要:Heydt, H., Science of Synthesis Knowledge Updates, (2014) 3, 417.