发明名称 NEW PRODUCTION INTERMEDIATE OF FLUORINE-CONTAINING 1,4- DISUBSTITUTED PIPERIDINE DERIVATIVE
摘要 <p>PROBLEM TO BE SOLVED: To obtain a new compound having a highly selective muscarine M3 receptor antagonism, slight adverse effect and safety, effective for treating and preventing diseases related to muscarine M3 receptor such as chronic closed pulmonary disease, chronic bronchitis, etc. SOLUTION: This derivative is (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2- hydroxy-2-phenylacetic acid. The compound is shown by formula I [Ar is an aryl, a heteroaryl or the like; R1 is a (substituted) 3-6C cycloalkyl; R2 is a (substituted) 5-15C (un)saturated aliphatic hydrocarbon or the like; X is O or NH]. The compound is obtained by reacting a carboxylic acid of formula II [R10 is a (substituted) 3-6C cycloalkyl or the like] or its reactive derivative with a compound of formula III [R20 is a (substituted) 5-15C aliphatic hydrocarbon] or its salt and removing the protecting group.</p>
申请公布号 JP2000178231(A) 申请公布日期 2000.06.27
申请号 JP20000027461 申请日期 2000.02.04
申请人 BANYU PHARMACEUT CO LTD 发明人 TSUCHIYA YOSHIMI;NOMOTO TAKASHI;OSAWA KOICHI;KAWAKAMI KUMIKO;OWAKI KENJI;NISHIKIBE MASARU
分类号 C07C69/732;C07C59/115;(IPC1-7):C07C69/732 主分类号 C07C69/732
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