| 摘要 |
PROCESS FOR THE PREPARATION OF THIENO-PYRIDINE DERIVATIVES.. This invention relates to a process for the preparation of thieno-pyridine derivatives having the structural formula : (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 (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 : (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 (VI) and (c) subsequently cyclising compound (VI) with formaldehyde to give the derivative of the formula (I). |
