反应详情

Using the procedures described in example 16 step 16a 1-[(benzyloxy)carbonyl]piperidine-4-carboxylic acid (2.5 g) was transformed into 2.75 g of crude benzyl 4-(chlorocarbonyl)piperidine-1-carboxylate and the latter compound was coupled with 2-aminomethyl-3-chloropyrazine hydrochloride (content 77%; 2.28 g) to give benzyl 4-((3-chloropyrazin-2-yl)methylcarbamoyl)piperidine-1-carboxylate (3.08 g) after purification by column chromatography (silica gel, dichloromethane/methanol gradient 100/0 to 90/10).