PROCESS FOR PRODUCTION OF 5-CHLORO-2,4-DIHYDROXYPYRIDINE

摘要

A process for producing 5-chloro-2,4-dihydroxypyridine of Formula (1) comprising the steps of reacting a 5-chloro-1,3-dioxin-4-on derivative (2) represented by Formula (2) with a ketene acetal derivative (3) represented by Formula (3) to give a pyrone derivative (4) represented by Formula (4), treating the pyrone derivative (4) with an acid, and reacting the resulting product with ammonia: [Chemical formula 4] (1); [Chemical formula 1] (2) wherein R<SUB>1</SUB> and R<SUB>2</SUB> are as defined in the description; [Chemical formula 2] (3) wherein R<SUB>3</SUB> and R<SUB>4</SUB> independently represent a straight-chain or branched alkyl group having 1 to 6 carbon atoms or a silyl group substituted by a straight-chain or branched alkyl group having 1 to 6 carbon atoms; and [Chemical formula 3] (4) wherein R<SUB>3</SUB> and R<SUB>4</SUB> are as defined above. This process can produce 5-chloro-2,4-dihydroxypyridine which is an inhibitor of a biodegradation enzyme against an anti-malignant tumor agent 5-fluorouracil under mild conditions in a short process and generates less industrial waste, and therefore is industrially advantageous.