公开(公告)号：US4490292A

公开(公告)日：1984-12-25

申请号：US540000

申请日：1983-10-07

申请人： Yoshifumi Maki ,  Magoichi Sako ,  Naomichi Mitsumori ,  Sadayuki Maeda ,  Masahiro Takaya

发明人： Yoshifumi Maki ,  Magoichi Sako ,  Naomichi Mitsumori ,  Sadayuki Maeda ,  Masahiro Takaya

IPC分类号： C07D277/68 ,  C07D279/16 ,  C07D281/10 ,  C07D281/02

CPC分类号： C07D277/68 ,  C07D279/16 ,  C07D281/10 ,  Y10S514/821

摘要： Novel 1,5-benzothiazepine derivatives having the formula; ##STR1## (wherein R.sub.1, R.sub.2 and R.sub.3 each denotes hydrogen, a halogen, a lower alkyl group, a lower alkoxy group or a hydroxy group; R.sub.4 denotes a lower alkyl group, an allyl group, a lower alkoxyalkyl group, a lower alkyl group substituted with a hydroxy group or a halogen, a lower alkylaminoalkyl group or a morpholino lower alkyl group; X denotes a halogen or hydrogen) are produced from corresponding 1,4-benzothiazine by a ring expansion reaction with trimethylhalosilane, hydrogen peroxide and water. The derivatives have analgesic, antipyretic and antiarrythmic activities.

摘要翻译： 具有下式的新的1,5-苯并硫氮杂衍生物： （其中R1，R2和R3各自表示氢，卤素，低级烷基，低级烷氧基或羟基; R4表示低级烷基，烯丙基，低级烷氧基烷基，低级烷基 通过与三甲基卤代硅烷，过氧化氢和水的环膨胀反应，由相应的1,4-苯并噻嗪制备由羟基或卤素取代的基团，低级烷基氨基烷基或吗啉代低级烷基; X表示卤素或氢。 衍生物具有镇痛，解热和抗焦虑活性。