发明名称 PRODUCTION OF (2,4,5-TRIFLUORO-3-METHOXYBENZOYL) ACETIC ACID ESTER DERIVATIVE AND ITS PRODUCTION INTERMEDIATE
摘要 PROBLEM TO BE SOLVED: To obtain a benzoylacetic acid ester derivative in high yield by condensing the carboxylic acid of a methoxyphthalic acid monoester derivative with a malonic acid ester derivative to bring to be a benzoylmalonic acid ester derivative, hydrolyzing to lead to an acetylbenzoic acid form, successively decarbonating to lead to an acetophenone form, and further alkoxycarbonylating. SOLUTION: A benzoylacetic acid ester derivative (E), [e.g. ethyl 2,4,5- trifluoro-3-methoxybenzoyl) acetate, etc.], expressed by formula V (R4 is a lower alkyl) is obtained in high yield by condensing (A) the carboxylic acid in a methoxyphthalic acid monoester derivative expressed by formula I (R1 is a lower alkyl) with (B) a malonic acid ester derivative to lead to a benzoylmalonic acid ester derivative expressed by formula II (R2 and R3 are each a lower alkyl), hydrolyzing the compound of formula II to lead to (C) an acetylbenzoic acid form of formula III, decarbonating the compound of formula III to lead to (D) an acetophenone form of formula IV and alkoxycarbonylating the compound of formula IV.
申请公布号 JP2000119221(A) 申请公布日期 2000.04.25
申请号 JP19980292529 申请日期 1998.10.14
申请人 KYORIN PHARMACEUT CO LTD;SAGAMI CHEM RES CENTER 发明人 ASAHINA YOSHIKAZU;TERAJIMA ATSURO
分类号 C07C49/84;C07C67/313;C07C69/738;C07C69/92;(IPC1-7):C07C69/738 主分类号 C07C49/84
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