首页> 外国专利> 2,6-Methano-3-benzazocine derivs. - used as analgesics and narcotic antagonists, prepd. from methano-benzoquinoline derivs.

2,6-Methano-3-benzazocine derivs. - used as analgesics and narcotic antagonists, prepd. from methano-benzoquinoline derivs.

机译:2,6-Methano-3-benzazocine衍生。 -用作镇痛药和麻醉剂拮抗剂。由甲醇-苯并喹啉衍生。

摘要

Methano-benzazocines of formula (I) and their acid addn. salts are new:- In (Ie R is methyl, pentyl, 3-methylbutyl, 2-phenylethyl 2-cyclopropylethyl, 2-cyclobutylethyl or 2-cyclopentylethyl. Prepn. of methano-benzazocines of formula (V) in which one of R2, R'2, R"2 and R'"2 is OH comprises cleaving the alkoxy gp. of a cpd. (V) in which one of R2, R'2, R'"2 is lower alkoxy. In the formula R1 is H, alkyl, alkenyl, alkynyl or haloalkenyl; cycloalkyl, cycloalkyl, alkyl; 2- or 3- furylmethyl (opt. ring substd. by 1-3 methyl or opt. ring-substd. phenyl-alkyl gps., or by 1 or 2 halogen, alkyl, alkoxy, alkanoyloxy or alkylthio, OH CF3 NH2 or alkanoylamino gps. or by one methylenedioxy gp.; one of R2, R'2, R"2, and R'"2 is OH or alkoxy and the others are H, or two adjacent gps. may be methylenedioxy; R3 is H or alkyl. R4 is H, alkyl, alkoxyalkyl, hydroxyalkyl alkylthioalkyl, alkylsulphinylalkyl, phenylthioalkyl, phenyl-sulphinylalkyl, alkenyl or haloalkyl; or R3 and R4 together are (CH2)m (n=3 or 4); R5 is alkylthioalkyl, alkoxyalkyl, lower alkoxy, cycloalkyl cycloalkyl-alkyl or Ar-(CH2)m; Ar is 2- or 3-aryl opt. substd. by 1-3 Me gps. or is phenyl opt. monosubstd. by methylenedioxy or mono- or disubstd. by halogen, alkyl, OH, alkanoyloxy, alkoxy, alkylthio, CF3, NH2 or alkanoylamino gps. m is 0, 2, 3 or 4 all alkyl etc. gps. are lower.
机译:式(I)的甲基苯甲唑啉及其酸加成。盐是新的:-(其中R是甲基,戊基,3-甲基丁基,2-苯基乙基2-环丙基乙基,2-环丁基乙基或2-环戊基乙基。 R′2,R″ 2和R′″ 2是OH,包括裂开Cdd(V)的烷氧基​​gp。其中R2,R′2,R′″ 2之一是低级烷氧基。 H,烷基,烯基,炔基或卤代烯基;环烷基,环烷基,烷基; 2-或3-呋喃基甲基(环优选被1-3个甲基取代或环优选被苯基烷基gps取代,或被1或2个卤素,烷基,烷氧基,烷酰氧基或烷硫基,OH CF3 NH2或烷酰氨基gps。或一个亚甲二氧基gp。; R2,R'2,R''2和R'''2中的一个是OH或烷氧基,另一个是H或两个相邻的gps可为亚甲二氧基; R3为H或烷基.R4为H,烷基,烷氧基烷基,羟烷基烷基硫代烷基,烷基亚磺酰基烷基,苯硫代烷基,苯基-亚磺酰基烷基,烯基或卤代烷基;或R3和R4一起为(CH2)m (n = 3或4); R5为烷硫基烷基,烷氧基烷基,低级烷氧基,c环烷基-环烷基-烷基或Ar-(CH2)m; Ar是2-或3-芳基选择。取代1-3 Me gps。或者是苯基选择。单价。通过亚甲二氧基或单或双键。通过卤素,烷基,OH,烷酰氧基,烷氧基,烷硫基,CF 3,NH 2或烷酰氨基gps。 m为0、2、3或4全烷基等。gps。较低。

著录项

  • 公开/公告号FR2460298B1

    专利类型

  • 公开/公告日1982-12-03

    原文格式PDF

  • 申请/专利权人 STERLING DRUG INC;

    申请/专利号FR19790016724

  • 发明设计人

    申请日1979-06-28

  • 分类号C07D221/26;

  • 国家 FR

  • 入库时间 2022-08-22 10:01:35

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号