发明申请
- 专利标题: PROCESS FOR PRODUCTION OF PIPERIDINE DERIVATIVES
- 专利标题(中): 生产哌啶衍生物的方法
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申请号: US12686516申请日: 2010-01-13
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公开(公告)号: US20100137605A1公开(公告)日: 2010-06-03
- 发明人: Thomas E. D'Ambra , Garry M. Pilling
- 申请人: Thomas E. D'Ambra , Garry M. Pilling
- 申请人地址: US NY Albany
- 专利权人: Albany Molecular Research, Inc.
- 当前专利权人: Albany Molecular Research, Inc.
- 当前专利权人地址: US NY Albany
- 主分类号: C07D211/34
- IPC分类号: C07D211/34
摘要:
The present invention is directed to a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-α,α-dimethyl-α-(4,4-dimethylisoxazolin-2-yl) toluene with N,N-dimethyl cyclopropylcarboxylic acid amide to provide 4-(cyclopropyl-oxo-methyl)-α,α-dimethyl-α-(4,4-dimethyloxozolin-2-yl) toluene; (2) hydrolyzing said 4-(cyclopropyl-oxo-methyl)-α,α-dimethyl-α-(4,4-dimethyloxozolin-2-yl) toluene to provide 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate with 4-(α,α-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate; (5) reducing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate; and (6) hydrolyzing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate to provide said 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid.
公开/授权文献
- US08476445B2 Process for production of piperidine derivatives 公开/授权日:2013-07-02
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