发明申请
- 专利标题: Process for the preparation of adapalene
- 专利标题(中): 阿达帕林制备方法
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申请号: US11392909申请日: 2006-03-30
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公开(公告)号: US20060229465A1公开(公告)日: 2006-10-12
- 发明人: Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Mauro Ercoli
- 申请人: Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Mauro Ercoli
- 优先权: ITMI2005A000550 20050401
- 主分类号: C07C69/76
- IPC分类号: C07C69/76
摘要:
A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.
公开/授权文献
- US07345189B2 Process for the preparation of adapalene 公开/授权日:2008-03-18
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