反应详情

A solution of (5-(4-fluorophenyl)-2-methylthiazol-4-yl)(1-(hydroxymethyl)hexahydrocyclopenta[c]pyrrol-2(1H)-yl)methanone (1 eq), phthalimide (2 eq) and triphenylphosphine (3 eq) in THF (56 mL) was cooled to 0° C. and added with DIAD (5 eq) dropwise. The resulting suspension was allowed to warm to rt gradually and stirred overnight, concentrated in vacuo to a brown oil. The reaction mixture was diluted with EtOAc and washed with water, brine, dried (MgSO4), and concentrated. The crude residue was purified by chromatography on silica gel (EtOAc/hex) to give the title compound as a clear oil. MS (ESI) 490.4 (M+H).

1. concentrationconcentrated in vacuo to a brown oil
2. additionThe reaction mixture was diluted with EtOAc
3. washwashed with water, brine
4. dry with materialdried (MgSO4)
5. concentrationconcentrated
6. customThe crude residue was purified by chromatography on silica gel (EtOAc/hex)