Trimethyl orthoformate → 5-amino-1-[2,6-dichloro4-(trifluoromethyl)phenyl]-3-[(1,1-dimethoxy)ethyl]4-methylthio-1H-pyrazole

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Reaction Conditions

Reaction Steps

A mixture of 2.0 g (0.0052 mole) of 3-acetyl-5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-methylthio-1H-pyrazole, 1.7 ml (0.0156 mole) of trimethyl orthoformate, 0.060 g (0.0003 mole) of para-toluenesulfonic acid monohydrate and 10 ml of methanol was heated at 40° C. for about 8 hours, then left 64 h at 20° C. The mixture was mixed with a saturated solution of NaHCO3, extracted with dichloromethane, and successively dried, filtered, evaporated, chromatographed on silica gel. 0.59 g of the title compound having a melting point of about 149° C. was obtained.

Provenance & Evidence