| 摘要 |
FIELD: chemistry. ^ SUBSTANCE: this invention refers to new production method of composition of formula I where R1 represents: H; cyano; optionally unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl group; or -C(O)-R5, where R5 represents H; optionally unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl group; either OR6 or NR6R7 where each R6 and R7 independently represents H optionally unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl group; R2 represents H; R3 represents H or alkyl; R4 represents H, halogen or alkyl including: a) Sonogashira coupling of formula II , where X represents halogen or CF3SO2-O- with compound of formula III to produce compound of formula IV ; b) reduction of connection of formula IV to produce compound of formula V ; c) transformation of compound of formula V into compound of formula VI ; d) N,N-dimethyl-2-nitroethylenamine treatment of compound of formula VI to produce compound of formula VII ; e) reduction of connection of formula VII to produce compound of formula VIII ; f) of compound of formula VIII by Raney-nickel reduction and subsequent base ring formation into compound of formula I. Besides described is production method of 8-fluorine-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indole-6-one through key Sonogashira coupling reaction and CuI-promotor indole production. ^ EFFECT: new production method of compounds of formulas I effective as poly(ADP-ribose)polymerase inhibitors is developed. ^ 8 cl, 13 ex |
