Title:
4-アミノ-4-フェニルピペリジン類の製造方法
Document Type and Number:
Japanese Patent JP4441260
Kind Code:
B2
Abstract:
The invention relates to a process for preparing a 4-amino-4-phenylpiperidine (I): in which R is hydrogen or a (C1-C3)alkyl group, characterized in that a 1-protected 4-piperidone (II): in which Pr' represents a removable N-protecting group, is treated sequentially first with an alkali metal cyanide and then with an amine ENHPr'' (III) in which E represents a group R'=(C1-C3)alkyl, or an N-protecting group and Pr'' is an N-protecting group, the protecting group(s) being removable under the same conditions as Pr'; then the compound thus obtained (IV) is subjected to a Grignard reaction with a phenylmagnesium halide, the two or three protecting groups are removed from the compound thus obtained (V) and compound (I) is isolated or in the form of the free base, which is converted into one of its salts.
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Inventors:
Alan Card, Alan
Anne-Arshard, Jill
Capro, Daniel
Anne-Arshard, Jill
Capro, Daniel
Application Number:
JP2003513942A
Publication Date:
March 31, 2010
Filing Date:
July 15, 2002
Export Citation:
Assignee:
Sanofi-Aventis
International Classes:
C07D211/66; C07D211/58; C07D211/68
Foreign References:
| GB1052302A |
Other References:
Bioorganic & Medicinal Chemistry Letters,1996年,Vol.6, No.19,pp.2307-2310
Attorney, Agent or Firm:
Shintaro Nogawa