PRODUCTION OF 2-(1H-1,2,4-TRIAZOL-1-YL)ACETOPHENONE

• Main Authors: MUROTANI YOSHIHARU, SAITO AKITO, KOMATSU MIWAKO, SHIMADA HITOYOSHI
• Format: Patent
• Language: English
• Published: 06.08.1996
• Edition: 6
• Subjects: CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

PURPOSE: To simply obtain a 2-(1H-1,2,4-triazol-1-yl)acetophenone, a raw material for producing antifungal agents and agrochemicals, in high yield and in a short time by de-esterifying and decarbonating a derivative obtained by reacting a reactive derivative of a benzoic acid with a triazole acetic acid derivative. CONSTITUTION: This method for producing 2-(1H-1,2,4-triazol-1-yl)acetophenone comprises de-esterifying and decarbonating (A) a 3-phenyl-2-(1H-1,2,4-triazol-1-yl) propionic acid ester derivative of formula I (R is a carboxyl-protecting group; R and R are each H, a lower alkyl, a lower alkoxy, cyano or nitro) to obtain (B) a 2-(1H-1,2,4-triazol-1-yl)acetophenone of formula II. The compound of the formula I can be obtained by reacting a 1,2,4-triazole acetic acid derivative of formula III with a reactive derivative of a benzoic acid of formula IV in the presence of a base and a metal halide.