Ethyl (R)-3-((((S)-1-Amino-1-Oxobutan-2-yl)Amino)Methyl)Hexanoate置于溶剂黄146体系中,用 四氢呋喃 用作溶剂,化学反应 4.0H,以28 G的收率获得布瓦西坦 参考文献: An Improved Process For The Preparation Of (2S)-2-[(4R)-2-Oxo-4-Propyltetrahydro-1H-Pyrrol-1-Yl] Butanamide And Its Intermediates Thereof[fr] Procédé Amélioré Pour La Préparation De (2S)-2-[(4R)-2-Oxo-4-Propyltétrahydro-1H-Pyrrol-1-Yl]Butanamide Et De Ses Intermédiaires 标题: An Improved Process For The Preparation Of (2S)-2-[(4R)-2-Oxo-4-Propyltetrahydro-1H-Pyrrol-1-Yl] Butanamide And Its Intermediates Thereof[fr] Procédé Amélioré Pour La Préparation De (2S)-2-[(4R)-2-Oxo-4-Propyltétrahydro-1H-Pyrrol-1-Yl]Butanamide Et De Ses Intermédiaires 摘要:本发明涉及一种改进的制备(2S)-2-[(4R)-2-氧代-4-丙基四氢-1H-吡咯-1-基]丁酰胺化合物的方法,其化学式为1,以及该化合物的中间体,中间体的新型盐化合物.此外,本发明还涉及新型盐在制备化合物1中的应用.本发明还涉及制备化合物1的新型方法.
专利号:US-11247977-B2 优先权日:2018-06-22 标题 :Compound and use thereof in synthesis of brivaracetam intermediate and crude drug 发明人:FENG YAN; WANG RUYONG; YE YIZHANG; ZHANG FENGSEN; GONG XUAN; WANG ZHONGHONG; KANG XINSHAN 权利人:FUJIAN HAIXI PHARMACEUTICALS CO LTD 摘要:The present application provides a compound in formula III, and further provides a use of the compound in the synthesis of a Brivaracetam intermediate and a crude drug, and a synthesis method. A raw material involved in the method of the present application is low in costs and easily available; (R)-4-propyl-dihydrofuran-2-ketone having high optical purity can be prepared; complicated separation and purification steps are avoided; costs are reduced, and the method is more applicable to industrial production.
专利号:US-2023183177-A1 优先权日:2020-04-24 标题:Enantioselective chemo-enzymatic synthesis of optically active amino amide compounds 发明人:GRILL BIRGIT; WINKLER MARGIT; SCHWAB HELMUT; STROHMEIER GERNOT; DONSBACH KAI; WALDVOGEL SIEGFRIED R; ARNDT SEBASTIAN; WEIS DOMINIK 权利人:PHARMAZELL GMBH 摘要:The present invention relates to a novel biocatalytic process for the stereoselective preparation of alpha amino amide compounds catalyzed by NHase enzymes. A further aspect of the invention relates to novel NHase enzymes as well as further improved NHase enzyme mutants, nucleic acid molecules encoding these enzymes, recombinant microorganisms suitable for preparing such enzymes and mutants. Another aspect of the invention relates to a chemo-biocatalytic process for the preparation of lactam compounds comprising the new catalytic process for the preparation of alpha amino amide compounds catalyzed by NHase enzymes, as well as the chemical oxidation of the alpha amino amide by applying certain chemical oxidation catalysts suitable for converting the alpha amino amide under retention of its stereochemical configuration to the respective lactam. The novel chemo-biocatalytic process is particularly suited for the synthesis of valuable pharmaceutical compounds, like in particular (S)-Levetiracetam.
专利号:US-2022064111-A1 优先权日:2019-01-17 标 题:Enantioselective synthesis of brivaracetam and intermediates thereof 发明人:ROY SARABINDU; GHOSH ANGSHUMAN; KUBEER RAMESH DHONDI; PRASAD MUTYALA V V VARA; PAUL GOPAL; GARAI ABHISHEK; CHAKRABORTY SOURAV; HALDAR ANIMESH; YADAW AJAY KUMAR; ROY SUBHO 权利人:CLININVENT RES PVT LTD 摘要:The present invention relates to an improved and economical process for enantioselective synthesis and purification of a novel key intermediate of Brivaracetam. Further, the present invention also relates to a process for the preparation of a chirally pure Brivaracetam of formula I utilizing the said intermediate.
专利号:US-11884623-B2 优先权日:2022-05-23 标题:Process for the preparation of (R)-4-propyl pyrrolidine-2-one, a key intermediate for synthesis of brivaracetam 发明人:DIVI MURALI KRISHNA PRASAD; BOLNENI NAGESWARA RAO; BANDARUPALLI LEELA MAHESWARA RAO 权利人:DIVIS LABORATORIES LTD 摘要:A process for the preparation of (R)-4-propyl-pyrrolidine-2-one, is provided which includes enzymatic conversion of dimethyl 3-propyl pentanedioate selectively into (S)-3-(2-methoxy-2-oxoethyl) hexanoic acid using Novozyme's Promea® enzyme, amidation of (S)-3-(2-methoxy-2-oxoethyl) hexanoic acid, followed by ester hydrolysis to obtain (S)-3-(2-amino-2-oxoethyl) hexanoic acid having high chiral purity >99% and converting the amide to amine by Hofmann rearrangement and cyclization resulting in (R)-4-propyl-pyrrolidine-2-one. It is further converted to Brivaracetam by N-alkylation with 2-bromobutyric acid, esterification followed by enzymatic resolution.
专利号:US-8338621-B2 优先权日:2005-12-21 标题:Process for the preparation of 2-oxo-1-pyrrolidine derivatives 发明人:SURTEES JOHN; BOUVY DIDIER; THOMAS ANTOINE; COMBRET YVES; FRANK MICHAEL; SCHMIDT GUNTHER; DUCHENE GUY 权利人:SURTEES JOHN; BOUVY DIDIER; THOMAS ANTOINE; COMBRET YVES; FRANK MICHAEL; SCHMIDT GUNTHER; DUCHENE GUY; UCB SA 摘要:The present invention relates to alternative processes for the preparation of 2-oxo-1-pyrrolidine derivatives of formula (I) n n n n n n n n n n Particularly, the present invention relates to alternative processes for the synthesis of levetiracetam, brivaracetam and seletracetam.
专利号:WO-2025109528-A1 优先权日:2023-11-24 标题:Telescopic synthesis of brivaracetam 发明人:JAGTAP ASHUTOSH; RAUT CHANGDEV; MARATHE SUYOG; SABALE YOGESHWAR; KUMBHAR AJAY 权利人:PIRAMAL PHARMA LTD 摘要:The present invention relates to a telescoping process for the preparation of brivaracetam. The process according to the present invention is a cost effective process in that it avoids isolation of intermediates at every step (Formula (I)).
摘要:González-Granda, S.; Gotor-Fernández, V., Science of Synthesis, (2022) , 248. 摘要:21 CFR Sections 1308.11-1308.15 摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from https://cns.public.lu/en/legislations/textes-coordonnes/liste-med-comm.html. Dataset DOI:10.5281/zenodo.4587355