反应详情

The requisite 1-(6-bromonaphth-2-ylsulphonyl)-4-[4-(2-t-butyloxycarbonylaminoimidazol-4-yl)benzoyl]piperazine starting material was prepared by a coupling method exactly analogous to that described in Example 1, starting from 4(2-t-butyloxycarbonylaminoimidazol-4-yl)benzoic acid and 1-(6-bromonaphth-2-ylsulphonyl)piperazine, to give 1-(6-bromonaphth-2-ylsulphonyl)-4-[4-(2-t-butyloxycarbonylaminoimidazol-4-yl)benzoyl]piperazine as a colourless solid (after trituration with hot ethanol) (248 mg, 40% yield), m.p. 175-177° C., 1H NMR (d6DMSO) 1.5 ppm (s,9H), 3.0-3.1 ppm (broad s,4H), 3.4-3.7 ppm (broad s,4H), 6.6 ppm (s,2H), 7.3 ppm (d,2H), 7.4 ppm (s,1H), 7.7 ppm (d,2H), 7.8 ppm (t,2H), 8.2 ppm (t,2H), 8.4 ppm (s,1H), 8.45 ppm (s,1H); MS (M+H)+ 640/642 (w), (M+H-56)+ 584/585 (s), loss of C4H8.

1. customThe requisite 1-(6-bromonaphth-2-ylsulphonyl)-4-[4-(2-t-butyloxycarbonylaminoimidazol-4-yl)benzoyl]piperazine starting material was prepared by a coupling method exactly analogous to