| abstract |
PURPOSE: To provide an α-oxoacetoamide deriv. that has serotonine workable L receptor activity and is effective for the therapeutic procedure of the vomitting, gastrointestinal disorder, CNS disorder, cardiovascular disorder, etc. n CONSTITUTION: The compd. of formula I [R 1 is a group of formula II, formula III [X, Y are each H, halo, cyano, etc.; X is O, S, NR 4 (R 4 is H, a lower alkyl, etc.); R 5 is the same as R 4 or denotes (CH 2 ) n (n is 3 to 5), etc., R 2 is formula IV, formula V (p is 0, 1; q is 1 to 3; R 6 is a 1 to 7C alkyl), etc.; R 3 is H, a lower alkyl] or its pharmaceutically acceptable salts as individual isomers or an isomer mixture. For example, N-(1-azabicyclo[2,2,2]octa-3-yl)-1-methyl-α- oxo-3 indoleacetoamide. The compd. of the formula I is obtd. by bringing, for example, the compd. of formula IV (R 7 is a halogen) and the substd. amine of the formula NHR 2 R 3 into reaction in a solvent, such as methylene chloride. If the substd. amine described above is an acid salt, the reaction is executed in a two-phase solvent consisting of water and the org. solvent in the presence of the base. n COPYRIGHT: (C)1992,JPO |