Polycyclic amines useful as cerebrovascular agents
申请人:WARNER-LAMBERT COMPANY
公开号:EP0388977A2
公开(公告)日:1990-09-26
A novel series of polycyclic amine derivatives, of formula I
methods of making the compounds, novel intermediates, compositions containing them, and pharmaceutical compositions useful in the treatment and prevention of cerebrovascular disorders and useful as anesthetics or analgesics.
式 I 的一系列新型多环胺衍生物
制造这些化合物的方法、新型中间体、含有这些化合物的组合物,以及用于治疗和预防脑血管疾病和用作麻醉剂或镇痛剂的药物组合物。
Imidomethylation of C-nucleophiles using O-phthalimidomethyl trichloroacetimidate and catalytic amounts of TMSOTf
作者:Ibrahim A.I Ali、El Sayed H El Ashry、Richard R Schmidt
DOI:10.1016/j.tet.2004.04.011
日期:2004.5
The O-phthalimidomethyl trichloroacetimidate (1), as a latent aminomethylating agent, exhibits high electrophilicity towards a variety of C-nucleophiles in the presence of catalytic amounts of TMSOTf and mild reaction conditions. The nucleophiles include aromatics, alkenes and active methylene compounds 2-11 whereby a phthalimidomethyl group could be introduced to give compounds 12-22. Removal of the phthaloyl group gave the respective amines, beta-amino ketones, and beta-amino acids. The O-(trichloroacetamido)methyl trichloroacetimidate (35) was also found to be a good amidomethylating agent. (C) 2004 Elsevier Ltd. All rights reserved.
PANDEY, V. K., CURR. SCI., INDIA, 1981, 50, N 15, 678-680