PROCESS FOR PRODUCING 3-/HETEROCYCLIC-METHYL-OR-HETEROCYCLIC-THIO-METHYL/-4-OXO- -PHTALAZINYL-1-ACETIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

摘要

Chloromethyl group substituted heterocyclic compounds of the formulae IMAGE I +TR IMAGE II wherein X is O or S; Y together with the two carbons to which Y is attached forms phenyl, pyridyl or pyrimidyl, each of which may be substituted by R; R is one of iodo or trifluoromethylthio or one or two of fluoro, chloro, bromo, (C1-C4)alkyl, (C1-C4)alkoxy, (C1-C4)alkylthio, (C1-C4)alkylsulfinyl, (C1-C4)alkylsulfonyl or trifluoromethyl; and R1 is hydrogen or R, are prepared by reacting a bifunctional compound of the formulae IMAGE with a 2-chloro-1,1,1-tri(C1-C6)alkoxyethane. Most of the compounds of formulae I and II are novel. These compounds are intermediates of use in the preparation of compounds having pharmaceutical activity. The 2-chloro-1,1,1-tri(C1-C6)alkoxyethanes are prepared from the corresponding tri(C1-C6)alkoxyethanes by chlorination with N-chlorosuccinimide or with chlorine in pyridine and a chlorohydrocarbon cosolvent.