反应详情

Preferably, the [5-cyclohexyl-1-(2-cyclopentyl-2-oxo-ethyl)-2-oxo-1,2-dihydro-benzo[e][1,2,4]triazepin-3-yl]-acetic acid is reacted with thionyl chloride in situ, in an organic solvent such as acetonitrile, THF, MTBE, and the like, preferably acetonitrile; and then reacted with 3-(3-amino-phenyl)-2H-[1,2,4]oxadiazol-5-one as its corresponding HCl salt, in the presence of an organic base such as TEA, DIPEA, pyridine, and the like, preferably DIPEA; wherein the base is preferably present in an amount greater than or equal to about 2 equivalents; in the same organic solvent; to yield the 2-[5-cyclohexyl-1-(2-cyclopentyl-2-oxo-ethyl )-2-oxo-1,2-dihydro-benzo[e][1,2,4]triazepin-3-yl]-N-[3-(5-oxo-2,5-dihydro-[1,2,4]oxadiazol-3-yl)-phenyl]-acetamide, the compound of formula (Is).