CAS: 398489-26-4; Tert-Butyl 3-Oxoazetidine-1-Carboxylate

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N-Boc-3-羟基氮杂环丁烷置于n-甲基咪唑,Copper(L) Iodide,Abno,氧气体系中,用 N-甲基吡咯烷酮 用作溶剂,化学反应 1.0H,以92%的收率获得1-Boc-3-氮杂环丁酮
参考文献:Cui / Abno / Nmi催化好氧醇氧化的工艺开发
标题:Cui / Abno / Nmi催化好氧醇氧化的工艺开发
摘要:已经开发出一种用于需氧醇氧化的改进的cu /硝基甲苯催化剂体系,用于将官能化的伯醇和仲醇氧化为醛和酮,适用于分批和流水工艺.该催化剂已在> 50 G的批量反应中得到证明,解决了与先前报道的(meo Bpy)cu I / Abno / Nmi催化剂体系(meo Bpy = 4,4'-Dimethoxy-2,2'-联吡啶,Abno = 9-氮杂双环[3.3.1]壬烷n-氧基,Nmi =n-甲基咪唑).重要的催化剂改性方法包括更换[cu(mecn)4] Otf具有低成本的铜源cui,将abno的负载量降低至0.05-0.3 Mol%,并且使用nmi作为唯一的配体/添加剂(即无需meo Bpy).使用高闪点溶剂n-甲基吡咯烷酮可在以空气为氧化剂的间歇反应中安全操作.对于与升高的气压兼容的连续流应用,使用乙腈作用作溶剂可观测到更好的性能.
Doi:10.1021/acs.Oprd.5B00179

专利信息

专利号:WO-2019086469-A1
优先权日:2017-10-30
标 题:Process for the production of cobimetinib
发明人：NERKARARYAN KRISTINE; SARGSYAN KARINE; GHARIBYAN MARIAM; GASPARYAN NAIRI; MOVSISYAN MIKAYEL; HAFERKAMP SVEN; MELLOR ANNA; PORSTMANN FRANK
权利人:AZAD PHARMACEUTICAL INGREDIENTS AG
摘要:The present invention relates to a novel route of synthesis for the production of enantiomerically pure Cobimetinib, new intermediates in the synthesis of Cobimetinib and an amorphous Cobimetinib hemifumarate salt comprising a high salt content.

专利号:US-11584708-B2
优先权日:2018-03-29
标题 :Synthesis of (2S,3R,4R)-4,5-dihydroxyisoleucine and derivatives
发明人：KNITTEL CAROLINE; SIEGERT MARY-ANN; SÃœSSMUTH RODERICH; WINK CHRISTOPH; JAS GERHARD
权利人:HEIDELBERG PHARMA RES GMBH
摘要:The invention relates to a method for the preparation of a 4,5-dihydroxyisoleucine derivative comprising the steps of asymmetric Claisen rearrangement of a Z-aminocrotyl-glycin ester and subsequent kinetic resolution of the product diastereomer mix by acylase, and subsequent Sharpless dihydroxylation of the resulting 2-amino-3-methylpent-4-enoic acid derivative.

专利号:US-2014371464-A1
优先权日:2012-02-03
标 题:Process for the preparation of chiral isoxazoline azetidine derivatives as antiparasitic agents
发明人：BILLEN DENIS; GREENWOOD SEAN DAVID WILLIAM; STUK TIMOTHY LEE
权利人:ZOETIS LLC
摘要:The invention recites a chiral process for the synthesis of isoxazoline azetidine phenyl substituted derivatives of Formula (1) stereoisomers thereof, veterinarily acceptable salts thereof, processes for making, and their use as a parasiticide in an animal. The variables *, R 1a , R 1b , R 1c , R 2 , and R 3 are as described herein

专利号:US-9593126-B2
优先权日:2012-11-21
标题 :Synthesis of spirocyclic isoxazoline derivatives
发明人：GREENWOOD SEAN D W; STUK TIMOTHY L
权利人:ZOETIS SERVICES LLC
摘要:The invention recites an improved process for preparing spirocyclic isoxazoline derivatives of Formula (1) wherein “*â€?, R 1a , R 1b , and R 1c are as described herein.

专利号:US-6774125-B2
优先权日:1998-06-22
标 题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

专利号:US-6509331-B1
优先权日:1998-06-22
标题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
发明人：AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H
权利人:ELAN PHARM INC; LILLY CO ELI
摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.