(3R)-3-Aminopiperidine, 3-BOC protected → (R)-tert-butyl 1-(4-(2-bromo-5-fluorobenzyl)-6-methyl-5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)piperidin-3-ylcarbamate

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The mixture of 4-(2-bromo-5-fluorobenzyl)-6-methyl-3-(methylthio)-1,2,4-triazin-5(4H)-one (17, 180 mg, 0.523 mmol) and (R)-tert-butyl piperidin-3-ylcarbamate (208 mg, 1.04 mmol) was ground for 5 min and then heated in a tube under nitrogen atmosphere at 135° C. for 13 h. The mixture was separated by silica gel column, and eluted with 10-50% ethyl acetate in petroleum ether to give (R)-tert-butyl 1-(4-(2-bromo-5-fluorobenzyl)-6-methyl-5-oxo-4,5-dihydro-1,2,4-triazin-3-yl)piperidin-3-ylcarbamate (18). MS: m/z, 496 (100%, M+1), 498 (100%).

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