首页> 外国专利> Cpds. of formula (I):- where R = H, halogen, lower alkyl or CF3, R1 = H, lower alkyl or lower alkenyl, R2-R5 = or lower alkyl, n = 1,

Cpds. of formula (I):- where R = H, halogen, lower alkyl or CF3, R1 = H, lower alkyl or lower alkenyl, R2-R5 = or lower alkyl, n = 1,

机译:Cpds。式(I)的通式:-其中R = H,卤素,低级烷基或CF 3,R 1 = H,低级烷基或低级烯基,R 2 -R 5 =或低级烷基,n = 1,

摘要

Cpds. of formula (I):- where R = H, halogen, lower alkyl or CF3, R1 = H, lower alkyl or lower alkenyl, R2-R5 = H or lower alkyl, n = 1, 2, 3 or 4 and non-toxic acid addition salts thereof. Anti-depressants comparing favourably with imipramine and amitriptyline in an anti-tetrabenzine depression test in mice. 6-Cl-2-carboxy-indole (26 pts.), Et2O (500 pts.) and SOCl2 (50 pts.) are stirred 8 hrs. at room temp., then Et2O and excess SOCl2 are evaporated off to leave crude 6-Cl-2-chlorocarbonyl-indole. 10.7 pts. of this crude material in Et2O (100 pts.) are added dropwise with stirring and cooling to N-(2-NH2-Et)-morpholine (13 pts.) in Et2O (100 pts.) and the mixture is left 20 hrs. at room temp., then mixed with 2 N NaOH (50 pts.). 6-Cl-N-(2-morpholinoethyl)-2-indole-carboxamide (11.6 pts.),.
机译:Cpds。式(I)的通式:-其中R = H,卤素,低级烷基或CF 3,R 1 = H,低级烷基或低级烯基,R 2 -R 5 = H或低级烷基,n = 1、2、3或4,且非-其毒性酸加成盐。抗抑郁药在小鼠抗丁苯嗪抑郁试验中优于丙咪嗪和阿米替林。将6-Cl-2-羧基吲哚(26分),Et 2 O(500分)和SOCl 2(50分)搅拌8小时。在室温下,然后蒸出Et 2 O和过量的SOCl 2,留下粗制的6-Cl-2-氯羰基-吲哚。 10.7分搅拌下逐滴加入在Et 2 O(100 pts。)中的该粗物质,冷却至在Et 2 O(100 pts。)中的N-(2-NH2-Et)-吗啉(13 pts。),并将混合物放置20小时。在室温下,然后与2 N NaOH(50分)混合。 6-Cl-N-(2-吗啉代乙基)-2-吲哚甲酰胺(11.6分)。

著录项

  • 公开/公告号FR1602884A

    专利类型

  • 公开/公告日1971-02-08

    原文格式PDF

  • 申请/专利权人

    申请/专利号FRD1602884

  • 发明设计人

    申请日1967-04-14

  • 分类号A61K31/535;C07D413/12;

  • 国家 FR

  • 入库时间 2022-08-23 09:22:33

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