Process for the preparation of thieno-pyridine derivatives

Claim 1

Process for the preparation of thieno-pyridine derivatives having the formula: ##STR62## in which R 1 is a member selected from the group consisting of C 1-7 alkyl; phenyl lower alkylene; phenyl lower alkylene in which the phenyl is substituted with 1 to 3 substituents selected from the group consisting of lower alkyl, hydroxy, lower acyloxy, lower alkoxy, nitro and halogen; naphthyl lower alkylene; thienyl lower alkylene; diphenyl lower alkylene; phenyl hydroxy-lower-alkylene; phenyl hydroxy-lower-alkylene in which the phenyl is substituted with 1 to 3 substituents selected from the group consisting of lower alkyl, hydroxy, lower acyloxy, lower alkoxy, nitro and halogen; naphthyl hydroxy-lower-alkylene; thienyl hydroxy-lower-alkylene; and diphenyl hydroxy-lower-alkylene; R 2 is selected from the group consisting of hydrogen and lower alkyl; and R 3 is hydrogen, comprising: (a) reacting a derivative having the formula: ##STR63## in which R 2 and R 3 are as defined for formula (I) and X is selected from the group consisting of hydrogen, an alkali metal and a radical MgY in which Y represents halogen, with a halosulfonyl derivative having the formula: Hal -- SO.sub.2 -- R.sub.4 (III) in which Hal represents halogen and R 4 is selected from the group consisting of methane sulfonyl, trichloromethane sulfonyl, trifluoromethane sulfonyl, benzene sulfonyl, paratoluene sulfonyl, m. acetyl benzene sulfonyl and p. bromophenyl sulfonyl, to give a compound having the formula: ##STR64## (b) reacting said derivative (IV) with an amine of the formula R.sub.1 -- NH.sub.2 (V) in which R 1 is as defined for formula (I), to give a compound having the formula: ##STR65## and (c) subsequently cyclising said derivative (VI) with formaldehyde to give the derivative of the formula (I).