A variety of diazepinone derivatives were prepared from α-amino acids and amino alcohols by a new synthetic methodology based on ring closing metathesis as a key step. The diazepinones were coupled with ribose derivatives to afford novel diazepinone nucleosides. Among them,(4R)-1-ribosyl-4-methyl-3, 4-dihydro-1H-1, 3-diazepin-2 (7H)-one (3) showed a potent inhibitory effect (Ki= 145.97±4.87 nM) against human cytidine deaminase.
[Liu, Paul S.; Marquez, Victor E.; Driscoll, John S.; Fuller, Richard W.; McCormack, John J. Journal of Medicinal Chemistry, 1981 , vol. 24, # 6 p. 662 - 666]
