O[N:2]1[C:6]2[CH:7]=[CH:8][CH:9]=[CH:10][C:5]=2N=N1.Cl.C(N=C=NC[CH2:18][CH2:19]N(C)C)C.CN1CC[O:27]CC1.N.[O:31]1[CH2:35][CH2:34][CH2:33][CH2:32]1>>[OH:31][C:35]1[CH:19]=[CH:18][C:32]([C:7]2([C:6]([NH2:2])=[O:27])[CH2:8][CH2:9][CH2:10][CH2:5]2)=[CH:33][CH:34]=11-Hydroxybenzotriazole (3.68 g, Aldrich), 1-Ethyl-3-(3-Dimethylaminopropyl)-carbodiimide hydrochloride (5.28 g Sigma) and N-Methylmorpholine (2.78 g, Aldrich) were added, under nitrogen, to a stirred solution of the product from Example 4(a) (5.0 g) in dry tetrahydrofuran (THF). The mixture was stirred at RT for four hours, then slowly added to liquid ammonia (excess) at -60° C. After one hour, the mixture was warmed to RT and stirred overnight.
Loading…
