abstract |
The invention discloses a method for synthesizing a sulfentrazone intermediate and a sulfentrazone. The method comprises: 1-phenyl-3-methyl-1H-1,2,4-triazol-5-one as a raw material, under the action of compound (A) or compound (B) and a base, in the aprotic The sulfentrazone intermediate (III) is obtained in the solvent, and the intermediate (IV) is obtained by difluoromethylation. After chlorination, nitration, reduction, and mesylation, N-(2,4-dichloro -5-(4-Difluoromethyl-4,5-dihydro-3-methyl-5-oxo-1H-1,2,4-triazol-1-yl)phenyl)methanesulfonamide product. The beneficial effects of the present invention are mainly reflected in: using the catalytic hydrogenation process, the nitro reduction not only has high chemoselectivity, but also is greener, more efficient, safe and reliable, and the catalyst used in the sulfonylation reaction is triphenylphosphine, polyethylene glycol Or crown ether, instead of the previously used catalysts such as DMF, less side reactions and high yield. The overall process is simple and convenient, the reaction conditions are mild, the yield is high, and the product quality is high, which is beneficial to industrial production. |