氯化氰 反应生成2-(2-氯-1-亚乙基)酰肼甲酸甲酯 参考文献:Morpholine Compounds Are Prodrugs Useful As Tachykinin Receptor 标题:Morpholine Compounds Are Prodrugs Useful As Tachykinin Receptor 摘要:通用结构式为:##str1## 的替代杂环是一种在治疗炎症性疾病,疼痛或偏头痛,哮喘和呕吐方面有用的tachykinin受体拮抗剂.
专利号:US-6407255-B2 优先权日:1998-06-16 标题:Chemical synthesis of 1,2,4-triazolinone derivative 发明人:COTTRELL IAN FRANK; DOLLING ULF H; HANDS DAVID; WILSON ROBERT DARRIN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents.
专利号:US-8940890-B2 优先权日:2010-05-24 标 题:Preparation method of 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one 发明人:JI JIANXIN; ZHANG QIANG; DU FENGTIAN; JIN YI; ZHANG TAO; GUO NA; YAN XIAOWEI; YANG YONGRONGN; LI BOGANG 权利人:JI JIANXIN; ZHANG QIANG; DU FENGTIAN; JIN YI; ZHANG TAO; GUO NA; YAN XIAOWEI; YANG YONGRONGN; LI BOGANG; CHENGDU DI AO PHARMACEUTICAL GROUP CO LTD 摘要:Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C 1 -C 5 alkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.
专利号:US-2002019524-A1 优先权日:1998-06-16 标题 :Chemical synthesis of morpholine derivatives
专利号:US-6297376-B1 优先权日:1998-06-16 标题 :Chemical synthesis of morpholine derivatives