Title:
【発明の名称】抗精神病活性を有する2,3,4,5-テトラヒドロ-1H-3-ベンズアゼピンおよびα-置換アリールアセトアミドの合成
Document Type and Number:
Japanese Patent JPH07504196
Kind Code:
A
Abstract:
PCT No. PCT/US93/01425 Sec. 371 Date Aug. 19, 1994 Sec. 102(e) Date Aug. 19, 1994 PCT Filed Feb. 23, 1993 PCT Pub. No. WO93/16997 PCT Pub. Date Sep. 2, 1993.A novel process for the preparation of alpha -substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the alpha -carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R4-X, wherein R4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The alpha -substituted arylacetamides are useful as intermediates in the preparation (by reduction) of alpha -substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R4 is 1-(1-cycloalkenyl) are novel.
Inventors:
Joel Gee, Burger
Chan, Way Kay
Kozlowski, Joseph A.
Zo, Guoway
Chan, Way Kay
Kozlowski, Joseph A.
Zo, Guoway
Application Number:
JP51494393A
Publication Date:
May 11, 1995
Filing Date:
February 23, 1993
Export Citation:
Assignee:
SCHERING CORPORATION
International Classes:
A61K31/55; A61P25/00; A61P25/18; B01J31/24; C07B61/00; C07C231/12; C07D209/34; C07D217/24; C07D213/56; C07D223/16; C07D225/06; C07D233/64; C07D277/30; C07D307/54; C07D333/24; C07D491/056; (IPC1-7): C07D223/16; A61K31/55
Attorney, Agent or Firm:
Kyozo Yuasa (6 people outside)