Production of n-phenylacetic acid derivative of thetrahydrothieno(3,2-c)pyridine and its intermediate

PURPOSE: To produce stereospecifically the subject compound by rearing the reaction product of α-amino(2-chlorophenyl)methyl acetate and thienyl derivative, product with a formulation agent and cyclizing it in the presence of an acid. CONSTITUTION: The compound of formula II is obtained by reacting α-(2-thienyl amino) (2-chlorophenyl)methyl acetate with a formulation agent and chylizing the obtained reaction product in the presence of an acid. As formylation agent, formaldehyde, its hydrate or polymer, the compound of the formula XCH 2 Y (X is a halogen, 1-4C alkoxy, ≥1C alkylthio or NH 2 ; Y is a 1-4C alkoxy, 1-4C alkylthio, amino, 2-5C alkoxycarbonyl or phenoxycrbonyl) or heterocyclic compound of formula III (Z is O, NH or S) is used. The compound of the formula I is obtained by reacting the compound of the formula IV with the compound of the formula V [X is a halogen or RSO 2 (R is a 1-4C alkyl or phenyl)] in an inactive solvent in the presence of a base. COPYRIGHT: (C)1992,JPO