Process for the preparation of thienopyridine derivatives

Details Process for the preparation of thienopyridine derivatives Process for the preparation of thienopyridine derivatives

C - Chemistry, Metallurgy

07

D

260/276.1

C07D 495/04 (2006.01) C07D 333/16 (2006.01) C07D 333/20 (2006.01)

Patent

CA 1071630

PROCESS FOR THE PREPARATION OF THIENO-PYRIDINE DERIVATIVES. ABSTRACT OF THE DISCLOSURE. This invention relates to a process for the preparation of thieno-pyridine derivatives having the structural formula : Image (I) in which R1 represents an optionally subsituted alkyl, aryl or aralkyl radical, and R2 and R3 represent each hydrogen or a lower alkyl, aryl or heterocyclic radical, comprising : (a) reacting a derivative of the formula Image (II) in which R2 and R3 are as defined for formula (I) and X represents hydrogen, or an alkali metal, or a radical Mg-Y in which Y represents halogen, with a halo-sulfonyl derivative having the formula : Hal-SO2-R4 (III) in which Hal represents halogen and R4 represents an optionally substituted alkyl, aryl or aralkyl group, to give a compound having the formula : Image (IV) (b) subsequently reacting the latter compound with an amine of the formula : R1-NH2 (V) in which R1 is as defined for the formula (I), to give a compound having the ormula : Image (VI) and (c) subsequently cyclising compound (VI) with formaldehyde to give the derivative of the formula (I). - 1 -

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