Preparation method of 3-(2-chloro-pyrimidine-4-yl)-1-methylindole
A technology of methyl indole and chloropyrimidine, which is applied in the field of medicine, can solve the problems of high pollution after treatment and dangerous reaction, and achieve the effect of high yield, safety and easy cost
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[0022] Example 1: Preparation of 3-(2-chloropyrimidin-4-yl)-1-methylindole
[0023]
[0024] With 1.5L methanol, 3-(2-chloropyrimidin-4-yl)-1H-indole (229g), formaldehyde (90g), 10% palladium carbon (20g) was added in the reaction kettle, under hydrogen atmosphere (0.2MPa) , stirred at room temperature for 3 hours, the reaction was completed, filtered, the organic phase was evaporated to dryness, and recrystallized with acetonitrile to obtain the product 3-(2-chloropyrimidin-4-yl)-1-methylindole, 210g, yield: 86.4 %.
[0025] 1H NMR (400MHz, 25℃, DMSO-d6): 3.90(3H,s), 7.30(2H,pd), 7.54-7.60(1H,m), 7.82(1H,d), 8.38-8.44(1H,m ), 8.49(1H,s), 8.53(1H,d).
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