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

被引:0
作者
WELLER, HN
MILLER, AV
DICKINSON, KEJ
HEDBERG, SA
DELANEY, CL
SERAFINO, RP
MORELAND, S
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中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
4-Alkyl-1,2,4-oxadiazinones were prepared by regiospecific alkylation of the corresponding 4H-oxadiazinones, which were synthesized by a trimethylaluminum mediated cyclization reaction. Alkylation was regiospecific and generally facile; in one example, however, an unusual fragmentation 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.
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页码:1027 / 1038
页数:12
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