PROCESS FOR PRODUCTION OF THIOPHENE COMPOUND AND INTERMEDIATE THEREOF.

摘要

Disclosed is a novel process for producing a 2-aryl-3-hydroxy-4-substituted-carbonylthiophene compound, which is a compound useful as an intermediate for the production of a pharmaceutical agent or an agricultural agent or an intermediate for the production of the 2-aryl-3-hydroxy-4-substituted-carbonylthiophene compound. A 2-aryl-3-hydroxy-4-substituted-carbonylthiophene compound (7) can be produced by: reacting a 2-arylacetic acid ester compound represented by formula (1) [wherein R1 represents an aryl group or the like; R4 represents a C1-3 alkyl group or the like; and X represents a leaving group] with a thioacetic acid compound to produce a thioacetyl compound (3); reacting the thioacetyl compound (3) with a vinyl ketone compound to produce a γ-ketosulfide compound (5); cyclizing the γ-ketosulfide compound (5) under basic conditions to produce a dihydrothiophene compound (6); oxidizing the dihydrothiophene compound (6) with an oxidizing agent to produce the 2-aryl-3-hydroxy-4-substituted-carbonylthiophene compound (7). (1) (3) (5) (7) (7).