申请人:Mead Johnson & Company
公开号:US03946004A1
公开(公告)日:1976-03-23
Novel amidine compounds selected from the group consisting of bis-pyrrolinyl derivatives of phenothiazines, phenoxazines and acridans are obtained by reacting a phenothiazine, phenoxazine or acridan with a pyrrolidinone in the presence of phosphorus oxychloride. The phenothiazine, phenoxazine, or acridan can also be alkylated with 2-chloro-1-(1-pyrrolin-2-yl)-2-pyrroline to provide compounds of the invention. Typical examples of bis-pyrrolinyl derivatives are 2-methoxy-10-[5-methyl-1-(5-methyl-1-pyrrolin-2-yl)-2-pyrrolin-2-yl]-pheno thiazine, 10-[1-(1-pyrrolin-2-yl)-2-pyrrolin-2-yl]phenoxazine, and 9,9-dimethyl-10-[5-methyl-1-(5-methyl-1-pyrrolin-2-yl)-2-pyrrolin-2-yl]acr idan. The amidine compounds are useful as diuretics, smooth muscle relaxants and antithrombogenic agents.
从苯并噻嗪,苯并噁嗪和乙酰基蒽中选择的双吡咯烷衍生物中选出新型的氨基咪啉化合物。在磷酸氧氯化物的存在下,将苯并噻嗪,苯并噁嗪或乙酰基蒽与吡咯酮反应即可得到该化合物。苯并噻嗪,苯并噁嗪或乙酰基蒽也可以与2-氯-1-(1-吡咯烷-2-基)-2-吡咯烷烷基化,以提供本发明的化合物。双吡咯烷衍生物的典型例子是2-甲氧基-10-[5-甲基-1-(5-甲基-1-吡咯烷-2-基)-2-吡咯烷-2-基]-苯并噻嗪,10-[1-(1-吡咯烷-2-基)-2-吡咯烷-2-基]苯并噁嗪和9,9-二甲基-10-[5-甲基-1-(5-甲基-1-吡咯烷-2-基)-2-吡咯烷-2-基]乙酰基蒽。该氨基咪啉化合物可用作利尿剂,平滑肌松弛剂和抗血栓形成剂。