摘要 |
PROBLEM TO BE SOLVED: To obtain a new benzofuryl-α-pyridone derivative, whereα-pyridone group is substituted for denzofuryl one, useful as a lipid metabolism-improving agent, an arteriosclerosis-preventing agent, and especially useful as a triglyceride biosynthesis-inhibiting agent, an in-blood triglyceride-lowering agent or the like. SOLUTION: This new compound is expressed by the formula [wherein, R1 is H, a 7-20C aralkyl or the like; R2 is a 1-5C alkyl; R3 is H, CO-R6 (wherein, R6 is H, a heterocycle or the like) or the like; R4 is H, a 2-5C alkenyl or the like; R5 is R5a (wherein, R5a is H, nitro or the like) or the like, and a substituent located at the 4, 5, 6, or 7 position of benzofuran ring] and is, e.g. 6-[5-(3- pyridyl)methyloxybenzofuran-2-yl]-3,5-dimethyl-4-hydroxy-2H-pyrid-2-one. The compound of the formula is obtained, e.g. by treating a solution of a 2,4-two substitution-β-keto ester with a base to convert into a dienolate, by reacting it with a benozofurancarboxylate to form a diketo ester intermediate and by its alkaline hydrolysis, followed by the acid treatment of a product.
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