发明名称 |
PROCESS FOR THE PREPARATION OF 3,3-DISUBSTITUTED PIPERIDINES |
摘要 |
<p>A process for preparing a compound of formula (I), wherein R1 represents hydrogen or a protecting group; and R2 represents hydrogen or benzoyl optionally substituted in the phenyl moiety with halogen, methyl or C1-4 alkoxy; which process comprises cyclising a compound of formula (II), wherein R1 is as defined in relation to (I), to provide a cyclic lactam of formula (III), wherein R1 is as defined in relation to (I); reducing the compound of formula (III) so formed to provide a compound of formula (I) wherein R2 represents hydrogen; and thereafter carrying out one or more of the following optional steps: (a) N-acylating the compound of formula (I) wherein R2 represents hydrogen to provide a compound of formula (I) wherein R2 represents benzoyl wherein the phenyl moiety is optionally substituted with halogen, methyl or C1-4 alkoxy; and (b) removing any protecting group.</p> |
申请公布号 |
EP0915849(A2) |
申请公布日期 |
1999.05.19 |
申请号 |
EP19970937554 |
申请日期 |
1997.08.04 |
申请人 |
SMITHKLINE BEECHAM S.P.A.;SMITHKLINE BEECHAM CORPORATION |
发明人 |
GRUGNI, MARIO;RIGOLIO, ROBERTO;ERHARD, KARL, FRANCIS |
分类号 |
C07B57/00;C07D211/22;C07D211/58;C07D211/88;(IPC1-7):C07D211/22 |
主分类号 |
C07B57/00 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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