CAS: 199174-24-8; (S)-1-Boc-(3-Hydroxymethyl)Pyrrolidine

相似化合物

110013-18-8 110013-19-9 114214-69-6

上下游产品

CAS号173724-95-3 ((S)-1-((S)-1-苯... | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1264942-79-1 (3S)-3-({[tert-... | CAS号1123786-71-9 tert-butyl 2-(o... | CAS号140148-70-5 (S)-1-B°C-吡咯烷-3-甲酸 | CAS号109960-55-6 ((S)-1-((r)-1-苯... | CAS号114214-69-6 1-B°C-3-羟甲基吡咯烷 | CAS号617-52-7 衣康酸二甲酯 | CAS号99735-46-3 甲基 (3s)-5-氧亚基-1... | CAS号224168-68-7 3(S)-碘甲基吡咯烷-1-羧酸叔丁酯 | CAS号1067230-64-1 N-B°C-3(S)-溴甲基吡咯烷

衣康酸置于lithium Aluminium Tetrahydride,Palladium 10% On Activated Carbon,氢气体系中,用 2-甲基四氢呋喃,乙醇 用作溶剂,化学反应 92.0H,反应生成(S)-1-Boc-3-羟甲基吡咯烷
参考文献:合成和非肽α的绝对构型的确定v β 6整联蛋白拮抗剂的用于特发性肺纤维化治疗†
标题:合成和非肽α的绝对构型的确定v β 6整联蛋白拮抗剂的用于特发性肺纤维化治疗†
摘要:(S)-3-(3-(3-(3,5-二甲基-1 H-吡唑-1-基)苯基)-4-((R)-3-(2-(5,6,7),1,8-四氢-1,8-萘啶-2-基)乙基吡咯烷-1-基)丁酸(1),这是一种治疗特发性肺纤维化的潜在治疗剂,目前正处于i期临床试验中报告.合成的关键步骤包括将2-甲基萘吡啶与(R)-N-Boc-3-(碘甲基)-吡咯烷烷基化,以及不对称rh催化的芳基硼酸加成到4-(n-吡咯烷基)巴豆酸酯.七个线性步骤合成的总产率为8%,并且在> 99.5%ee和80%de的条件下获得了产物.的绝对构型1由一个替代不对称合成涉及使用伊文思恶唑烷酮化学,酰化使用所得2-Arylsuccinic酸和还原芳基乙酸的烷基化建立.苄基不对称中心的绝对构型被确定为(S).
Doi:10.1039/c6Ob00496B

专利信息

专利号:EP-1836163-B1
优先权日:2004-12-23
标题 :Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin
发明人：BREITENSTEIN WERNER; COTTENS SYLVAIN; EHRHARDT CLAUS; JACOBY EDGAR; LORTHIOIS EDWIGE LILIANE JEANNE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER; SIMIC OLIVER
权利人:NOVARTIS AG
摘要:Novel 3-mono-, 3,4-di- and 3,4,4,-tri-substituted pyrrolidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on inappropriate activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on inappropriate activity of renin; the use of a compound of that class in the treatment of a disease that depends on inappropriate activity of renin; pharmaceutical formulations comprising a said substituted pyrrolidine compound, and/or a method of treatment comprising administering a said substituted pyrrolidine compound, a method for the manufacture of said substituted pyrrolidine compounds, and novel intermediates and partial steps for their synthesis are described. The substituted pyrrolidine compounds are especially of the formula I wherein the substituents are as described in the specification.

专利号:US-9328138-B2
优先权日:2011-11-15
标题:HCV NS3 protease inhibitors
发明人：RUDD MICHAEL T; MCCAULEY JOHN; LIVERTON NIGEL; GRISÉ-BARD CHRISTIANE; BROCHU MARIE-CHRISTINE; CHARRON SYLVIE; AULAKH VIRENDER; BACHAND BENOIT; BEAULIEU PATRICK; ZAGHDANE HELMI; HAN YONGXIN; FERRARA MARCO; HARPER STEVEN; SUMMA VINCENZO; CHACKALAMANNIL SAMUEL; VENKATRAMAN SRIKANTH; SHAH UNMESH; VELAZQUEZ FRANCISCO
权利人:MERCK SHARP & DOHME; MSD ITALIA SRL; MERCK CANADA INC
摘要:The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.