公开(公告)号：US3892756A

公开(公告)日：1975-07-01

申请号：US32800673

申请日：1973-01-30

Applicant: ROUSSEL UCLAF

Inventor： NEDELEC LUCIEN ,  FRECHET DANIEL

IPC: C07D451/00 ,  C07D221/02 ,  C07D451/02 ,  C07D471/02 ,  C07F9/6561 ,  C07D39/00

CPC classification number: C07D451/02 ,  C07F9/6561

Abstract: Racemates and optically active isomers of a compound selected from the group consisting of a compound of the formula

WHEREIN R is selected from the group consisting of hydrogen, lower alkyl optionally substituted with a member of the group consisting of hydroxy and halogen, lower alkenyl, lower alkynyl, -(CH2)n - COCH3 where n is 0 or 1,

wherein X is selected from the group consisting of lower alkyl and optionally substituted phenyl, aralkyl of seven to eight carbon atoms, acyl of an organic carboxylic acid of one to six carbon atoms optionally substituted with

where m is an integer from 0 to 6 and X1 is selected from the group consisting of hydrogen and lower alkyl,

where p is an integer from 1 to 6 and X1 is as before and

wherein X2 is lower alkyl and R1 and R2 are individually selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, trifluoromethyl and dilower alkylamino and the non-toxic, pharmaceutically acceptable acid addition and quaternary ammonium salts thereof which have a stimulating effect on the central nervous system while possessing at the same time anticonvulsant activity and their preparation.

Abstract translation: 选自下列化合物的化合物的外消旋物和旋光异构体：式WHEREIN R的化合物选自氢，任选被羟基和卤素的低级烷基取代的低级烷基，低级烯基，低级 炔基， - （CH 2）n -COCH 3，其中n是0或1，O并原-C-OX，其中X选自低级烷基和任选取代的苯基，7至8个碳原子的芳烷基，有机 任选被X1 - （CH2）mN ANGLE X1取代的1至6个碳原子的羧酸，其中m是0至6的整数，X 1选自氢和低级烷基，X 1 - （CH 2）p N ANGLE X1 其中p是1至6的整数，X 1如前所述，O＆amp; Y 2 -CH 2 -P 2 G 2，其中X 2是低级烷基，R 1和R 2分别选自氢，卤素，低级烷基，低级烷氧基 ，三氟甲基和二元烷基 否和其具有对中枢神经系统的刺激作用同时具有抗惊厥活性及其制备的无毒的药学上可接受的酸加成盐和季铵盐。