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Title:
PROCESS FOR THE PREPARATION OF 3,3-DISUBSTITUTED PIPERIDINES
Document Type and Number:
WIPO Patent Application WO1998005640
Kind Code:
A3
Abstract:
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. 00000

Inventors:
GRUGNI MARIO (IT)
RIGOLIO ROBERTO (IT)
ERHARD KARL FRANCIS (US)
Application Number:
EP9704275W
Publication Date:
May 22, 1998
Filing Date:
August 04, 1997
Export Citation:
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Assignee:
SMITHKLINE BEECHAM S.P.A.
SMITHKLINE BEECHAM CORPORATION
GRUGNI, MARIO
RIGOLIO, ROBERTO
ERHARD, KARL, FRANCIS
International Classes:
C07B57/00; C07D211/22; C07D211/58; C07D211/88; (IPC1-7): C07D211/22; C07D211/58
Foreign References:
EP0673928A11995-09-27
EP0512901A11992-11-11
Other References:
E. TAGMANN ET AL.: "]ber in 3-Stellung basisch substituierte Pyrrolidin-, Piperidin- und Hexamethylenimin-Derivate" HELVETICA CHIMICA ACTA, vol. 35, no. 4, 16 June 1952, BASEL, CH, pages 1235-49, XP002048798
G.A.M. GIARDINA ET AL: "A reliable and efficient synthesis of SR 142801" BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 6, no. 19, October 1996, OXFORD, GB, pages 2307-2310, XP002043892
H.G. CHEN ET AL.: "A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist" BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 7, no. 5, March 1997, OXFORD, GB, pages 55-60, XP002055505
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