发明申请
US20130310592A1 PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES 有权
制备吡唑羧酸酰胺的方法

PROCESS FOR THE PREPARATION OF PYRAZOLE CARBOXYLIC ACID AMIDES
摘要:
The invention relates to a process for the preparation of 3-difluoromethyl-1-methyl-1 H-pyrazole-4-carboxylic acid (9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-yl)-amide by acylating the oxime oxygen of the compound of formula (VIII), in the presence of a solvent and an acylating agent of formula (XI) R 1C(X)—CI (XI); wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; and a) if R1 is chloro and the compound of formula (XI) was added to the compound of formula (VIII); reacting the so obtained product of formula (XIIa) wherein X is oxygen or sulfur; with the compound of formula (IX) b) if R1 is chloro and the compound of formula (VIII) was added to the compound of formula (XI); or R1 is C1-C6alkoxy, CH3—C(═CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; reacting the so obtained product of formula (XII) wherein X is oxygen or sulfur; R1 is chloro if X is oxygen or sulfur; or R1 is C1-C6alkoxy, CH3—C(═CH2)-0-, phenoxy or trichloromethoxy if X is oxygen; with the compound of formula (IX).
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