Title:
4-フェニル-1,2,3,6-テトラヒドロピリジンの誘導体の新規の製造方法及び用いられる中間体
Document Type and Number:
Japanese Patent JP4538114
Kind Code:
B2
Abstract:
4-Phenyl-5-hydroxy-1,2,3,6-tetrahydropyridine derivatives (I) are prepared from 4-phenyl-1,2,3,6-tetrahydropyridine (II). The preparation of 4-phenyl-5-hydroxy-1,2,3,6-tetrahydropyridine derivatives of formula comprises: (1) reacting a compound of formula (II) with an electrophilic halogenation agent to obtain a compound of formula (III); (2) reacting (III) with a halohydroxylating agent to obtain a compound of formula (IV); (3) reacting (IV) with a base to obtain a compound of formula (V); (4) reacting (V) with diastereoselective reduction agent to obtain a compound of formula (VI); and (5) reacting (VI) with a reducing agent to obtain a racemic cis compound (I) (6) reacting (I) with resolving agent to obtain the desired optical form of (I). R<1> = H or 1-8C alkyl; R<2>, R<4> = 1-4C alkyl; R<3> = 1-8C alkyl; and Hal = halo. An Independent claim is also included for the compounds of formulae (III), (IV), (V) and (VI).
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Inventors:
Francis brion
Christian Richard
Christian Richard
Application Number:
JP16964099A
Publication Date:
September 08, 2010
Filing Date:
June 16, 1999
Export Citation:
Assignee:
Aventis Pharma Societe Anonym
International Classes:
C07D211/42; C07B57/00; C07D211/70; C07D491/044; C07D493/04
Foreign References:
| WO1997042949A1 |
Attorney, Agent or Firm:
Axis International Patent Business Corporation
Motohiro Kurauchi
Motohiro Kurauchi