4-Toluenesulfonyl chloride → N-(2-aminophenyl)-5-[(4-methylphenyl)sulfonyl]-4,5,6,7-tetrahydro[1,3]-thiazolo[5,4-c]pyridine-2-carboxamide

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Reaction Conditions

Reaction Steps

Triethyl amine (1.0 eq) was added to solution of N-(2-aminophenyl)-4,5,6,7-tetrahydro[1,3]thiazolo[5,4-c]pyridine-2-carboxamide obtained in step VIII of example I (1.0 mmol) in 10 mL THF. The solution was cooled to 0° C. 4-Methyl-benzenesulfonyl chloride (1.0 mmol) was added slowly with continuous stirring. Reaction mixture was brought to room temperature and stirred for 2 h Reaction mixture was concentrated, diluted with water, extracted dichloromethane, washed with brine solution, and dried over anhydrous Na2SO4. Concentrated and purified by column chromatography to yield the title compound.

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