Chloromethyl heterocyclics

C - Chemistry – Metallurgy – 07 – D

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C07D 263/56 (2006.01) C07D 277/64 (2006.01) C07D 403/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 413/14 (2006.01) C07D 417/06 (2006.01) C07D 417/12 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 1293726

P.C. 7013 CHLOROMETHYL HETEROCYCLICS Abstract Chloromethyl group substituted heterocyclic compounds of the formulae or Image Image I 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 or Image Image with a 2-chloro-1,1,1-tri(Cl-C6)alkoxyethane. Most of the compounds of formulae I and II are novel. These compounds are intermediates of use in the prepration 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 chlorina- tion with N-chlorosuccinimide or with chlorine in pyridine and a chlorohydrocarbon cosolvent.

522156

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