CAS: 61312-87-6; 4-Isobutylpyrrolidin-2-One

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181289-23-6 61312-87-6 181289-23-6

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📜(R,S)-3-Iso-Butyl-4-Aminobutyric Acid置于三甲基硅烷化重氮甲烷体系中,用 甲醇,正己烷 作为反应溶剂,化学反应 0.5H,反应生成 4-异丁基-2-吡咯烷酮
参考文献:通过动态动力学拆分α-手性脂肪醛的不对称胺化,以获取立体互补的brivaracetam和pregabalin前体
标题:通过动态动力学拆分α-手性脂肪醛的不对称胺化,以获取立体互补的brivaracetam和pregabalin前体
摘要:在过去的几十年中,生物催化已经成为活性药物成分(api)不对称合成的必不可少且用途广泛的工具.在这种情况下,尤其是转氨酶(tas)已成功用于制备多种α-手性,光学纯胺,是api的重要组成部分.在这里,我们详细介绍了转氨酶的开发,该酶识别具有脂肪族残基的醛部分附近的α-手性中心,为抗癫痫药brivaracetam和pregabalin的新颖合成路线开辟了概念.转型通过动态动力学拆分(dkr)基于醛对映异构体的生物诱导外消旋作用,可实现外消旋底物的定量转化胺化.介质,底物和酶工程技术都可以以高光学纯度获得立体互补药物胺前体的(R)和(S)对映体.
DOI:10.1002/adsc.201701449

专利信息

专利号:WO-2016075082-A1
优先权日:2014-11-10
标题:Stereoselective reductive amination of alpha-chiral aldehydes using omega-transaminases for the synthesis of precursors of pregabalin and brivaracetam
发明人：ZEPECK FERDINAND; NERDINGER SVEN; KROUTIL WOLFGANG; FUCHS CHRISTINE; SIMON ROBERT
权利人:SANDOZ AG
摘要:The present invention relates to processes comprising a combined racemization and stereoselective reductive amination step in which an aldehyde compound of formula (I) is contacted with an (R)-selective ω-transaminase or an (S)-selective ω-transaminase to racemize the compound of formula (I) and obtain an amine compound of formula (II). These processes are useful for the preparation of precursors of pharmaceutically active agents such as brivaracetam and pregabalin.

专利号:US-2011190393-A1
优先权日:2008-06-03
标题:Novel and efficient method for the synthesis of an amino acid
发明人：GORE VINAYAK; GADAKAR MAHESHKUMAR; SHINDE DATTATREYA
权利人:GENERICS UK LTD
摘要:The present invention relates to a novel process for the preparation of γ-amino acids, such as (±)-3-(aminomethyl)-5-methyl-hexanoic acid (1), which is a key intermediate in the preparation of the potent anticonvulsant pregabalin, (S)-(+)-3-(aminomethyl)-5-methyl-hexanoic acid (2), and its analogues.

专利号:US-8772301-B2
优先权日:2009-12-18
标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
发明人：HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D
权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

专利号:US-8466297-B2
优先权日:2010-11-01
标 题:Manufacturing process for (S)-Pregabalin
发明人：SOUKUP MILAN
权利人:SOUKUP MILAN
摘要:The present invention relates to a novel manufacturing process and novel intermediates useful in the synthesis of pharmaceutically active compounds of general formula I used for treatment of epilepsy, neuropathic pain, anxiety and social phobia. The invention describes preparation of enantiomerically pure (S)-Pregabalin from chiral pyrrolidin-2-one of formula IV.

专利号:US-2007066846-A1
优先权日:2005-04-11
标题:Process for making (S)-Pregabalin
发明人：MAYMON ASHER; KANSAL VINOD K; HEDVATI LILACH
权利人:MAYMON ASHER; KANSAL VINOD K; HEDVATI LILACH
摘要:The invention encompasses processes for the synthesis of (S)-Pregabalin, (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid.

专利号:EP-3199525-A1
优先权日:2014-09-22
标题 :Method for asymmetrically catalyzed synthesis of nitropyrazole amide compound