SYNTHESIS OF N-ALKYL-1,2,4-OXADIAZINONES AS ANGIOTENSIN-II (AT1) RECEPTOR ANTAGONISTS

4-Alkyl-1,2,4-oxadiazinones were prepared by regiospecific alkylation of the corresponding 4H-oxadiazinones, which were synthesized by a tri methylaluminum mediated cyclization reaction. Alkylation was regiospec ific and generally facile; in one example, however, an unusual fragmen tation reaction occurred. A homochiral oxadiazineone was also prepared and alkylated under the described conditions. 4-Biphenylmethyl-1,2,4- oxadi-azinones were potent angiotensin-II receptor antagonists.