反应详情

(R)-1-(N-Benzyloxycarbonylpyrrolidin-2-yl)-3-hydroxypropene and 2-bromo-4-cyano-N-trifluoroacetylaniline were used. Column chromatography using elution with a gradient of diethyl ether (5%-100%) in methylene chloride afforded the title compound as a clear, colorless oil: IR (CHCl3) 2231, 1702, 1157 cm-1 ; LRMS (m/z, relative intensity) 537 ([MH+ with 81Br], 13), 535 ([MH+ with 79Br], 13), 402 (29), 400 (30), 294 (55), 292 (57), 244 (80), 213 (89), 91 (100); Anal. calcd for C24BrF3H21N3O3 ·0.2 H2O: C, 53.39; H, 3.99; N, 7.78. Found: C, 53.25; H, 3.95; N, 7.98.

1. washelution with a gradient of diethyl ether (5%-100%) in methylene chloride