反应详情

The title compound was prepared by treating the product of Example 1 step (c) (0.2 g) in dry THF (10 ml) with methyl acetimidate hydrochloride (75 mg) followed by triethylamine (0.1 ml) and stirring overnight. The reaction mixture was poured into water and extracted with ethyl acetate. The extract was evaporated and the residue purified by chromatography (silica, 2–20% 7M ammonia in methanol/dichloromethane as eluent) to give a glassy solid. The solid was dissolved in methanol (10 ml), treated with 1M HCl in ether (1 ml) then evaporated. The residue was triturated with ether to give the title compound as a cream solid (90 mg). M.p. 133–135° C.

1. customThe title compound was prepared
2. extractionextracted with ethyl acetate
3. customThe extract was evaporated
4. customthe residue purified by chromatography (silica, 2–20% 7M ammonia in methanol/dichloromethane as eluent)
5. customto give a glassy solid
6. customthen evaporated
7. customThe residue was triturated with ether