(7R)-7-({[t-Butyl(dimethyl)silyl]oxy}methyl)-7-methyl-5-(methylthio)-2,3,6,7-tetrahydro-1,4-thiazepine → (8R)-8-({[Tert-butyl(dimethyl)silyl]oxy}methyl)-8-methyl-3-{1-[4-(2-methylpyrimidin-5-yl)phenyl]cyclopropyl}-5,6,8,9-tetrahydro[1,2,4]triazolo[4,3-d][1,4]thiazepine

Participants

Reaction Steps

A solution of the compound (591 mg, 2.23 mmol) obtained in Example 88-1) and the compound (750 mg, 2.35 mmol) obtained in Example 4-1) in t-butanol (10 mL) was stirred for 7 h under reflux conditions. The obtained reaction mixture was cooled to room temperature and concentrated under reduced pressure, and then the residue was purified by silica gel column chromatography (methanol:ethyl acetate=10:90 to 100:0) to obtain the title compound (861 mg, 70%) as a light yellow solid.

Provenance & Evidence