反应详情

In an analogous procedure to Example 651, part c, N*7*-(2,2-Difluoro-ethyl)-6,7,8,9-tetrahydro-5H-benzocycloheptene-2,7-diamine was combined with (1S,2S,3R,4R)-3-(2,5-Dichloro-pyrimidin-4-ylamino)-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid amide to yield (1S,2S,3R,4R)-3-{5-Chloro-2-[7-(2,2-difluoro-ethylamino)-6,7,8,9-tetrahydro-5H-benzocyclohepten-2-ylamino]-pyrimidin-4-ylamino}-bicyclo[2.2.1]hept-5-ene-2-carboxylic acid amide (54.09 mg, 51.7% yield) as a white powder. 1H-NMR (CDCl3) δ 7.86 (s, 1H), 7.40 (d, J=8.2 Hz, 1H), 7.28 (m, 1H), 7.01 (d, J=8.1 Hz, 1H), 6.88 (s, 1H), 6.82 (t, J=8.9 Hz, 1H), 6.31 (m, 2H), 5.83 (m, 1H), 5.56 (br s, 1H), 5.40 (br s, 1H), 4.36 (m, 1H), 3.05 (m, 3H), 2.89 (s, 1H), 2.78 (m, 3H), 2.47 (d, J=8.1 Hz, 1H), 2.24 (d, J=9.3 Hz, 1H), 2.07 (m, 2H), 1.63 (d, J=9.4 Hz, 1H), 1.31 (m, 2H). LC/MS (ESI+)=503 (M+H). MP=166° C.