摘要
用1-苄基-4-哌啶醇和二苯甲基溴经缩合、脱苄置换和水解反应制得4-二苯甲氧基哌啶,再与4-氯-1-(4-叔丁基苯基)-1-丁酮在碘化钾存在下缩合、成盐制得富马酸依巴斯汀,总收率36%。
A new H1-receptor antagonist ebastine was synthesized from 1-benzyl-4-piperidinol by condensation withPh2CHBr, debenzylation, replacement and hydrolytic decarboxylation to give 4-benzhydryloxypiperidine followed byreaction with 1-(4-t-butylphenyl)-4-chloro-butan-1-one and salt formation with fumaric acid in an overall yield of 36%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2004年第6期326-327,共2页
Chinese Journal of Pharmaceuticals
