期刊
SYNTHESIS-STUTTGART
卷 54, 期 3, 页码 658-666出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/a-1649-5317
关键词
[1,4]diazepinones; fused imidazolinium moiety; hydrated imidazoline ring expansion; 2-aminoethyl side chain expulsion; selective dopamine D-2 ligands
资金
- Russian Science Foundation [19-75-30008]
Attempts to extend the hydrated imidazoline ring expansion strategy to a series of diarene-fused [1,4]diazepinones did not lead to ring expansion but resulted in expulsion of the 2-aminoethyl side chain. This setback led to the discovery of selective dopamine D-2 ligands with elements of structure-activity relationships.
Attempts to extend the hydrated imidazoline ring expansion (HIRE) strategy to a series of diarene-fused [1,4]diazepinones (earlier applied successfully to bis-pyrido substrate nevirapine) did not result in ring expansion but, rather, led to 2-aminoethyl side chain expulsion. This seeming setback (setting the limitations to the HIRE methodology substrate scope) led to the discovery of selective dopamine D-2 ligands with elements of structure-activity relationships.
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