申请人:A. H. Robins Company, Incorporated
公开号:US04031245A1
公开(公告)日:1977-06-21
Novel alkenyl- and alkanylamines having the formula: ##STR1## wherein Am is lower-alkylamino, di-lower-alkylamino and piperidino; A is methylene and methylidyne; R is hydrogen, lower-alkyl, lower-alkoxy, halogen and trifluoromethyl; m is zero and one; n is one and two; X is halogen and the pharmaceutically acceptable acid addition salts thereof. The alkenylamines are prepared by contacting 1-cyclopropyl-1-phenyl-.omega.-amino-1-alkanols with strong mineral acids. The alkanylamines are prepared by hydrogenation of the alkenylamines. Some of the compounds exhibit potent antagonism to the depressant effects of tetrabenazine.
具有以下公式的新型烯丙基和烷基胺:##STR1## 其中,Am是低烷基氨基,二低烷基氨基和哌啶基;A是亚甲基和甲基亚甲基;R是氢,低烷基,低烷氧基,卤素和三氟甲基;m为零和一;n为一和二;X为卤素及其药学上可接受的酸盐。通过将1-环丙基-1-苯基-ω-氨基-1-脂肪醇与强矿酸接触制备烯丙基胺。通过烯丙基胺的氢化制备烷基胺。其中一些化合物表现出对四苯异azine的抑制作用的强效拮抗作用。