发明名称 Method of making (1S, 4R)-1-azabicyclo[2.2.1]heptan-3-one and (1R, 4S), 1-azabicyclo[2.2.1]heptan-3-one
摘要 PCT No. PCT/US98/01413 Sec. 371 Date Sep. 29, 1999 Sec. 102(e) Date Sep. 29, 1999 PCT Filed Jan. 27, 1998 PCT Pub. No. WO98/32759 PCT Pub. Date Jul. 30, 1998Racemic (+/-)-1-azobicyclo[2.2.1]heptan-3-one may be efficiently resolved into its (1S,4R)- and (1R,4S)-1-azabicyclo[2.2.1]heptan-3-one isomers by formation of di-p-toluoyl hemitartrate salts by combination with di-p-toluoyl-L-tartaric acid and di-p-toluoyl-D-tartaric acid, respectively. Selective crystallization using one of the di-p-toluoyltartaric acids in less than stoichiometric amount in a suitable solvent mixture allows isolation of the desired isomer as its respective di-p-toluoyl hemitartrate in high isomeric purity. The isolated hemitartrates are storage stable and may be used as such in the preparation of pharmaceuticals and other biologically active compounds, or may be used to provide the free base of the respective 1-azabicyclo[2.2.1]heptan-3-one isomer.
申请公布号 US6121306(A) 申请公布日期 2000.09.19
申请号 US19990355225 申请日期 1999.09.29
申请人 WARNER-LAMBERT COMPANY 发明人 SOBIERAY, DENIS MARTIN
分类号 A61K31/439;A61K31/192;A61K31/194;A61K31/4015;A61P25/28;C07D209/52;C07D487/08;(IPC1-7):A61K31/192;A61K31/401 主分类号 A61K31/439
代理机构 代理人
主权项
地址