期刊
PURE AND APPLIED CHEMISTRY
卷 85, 期 6, 页码 1079-1087出版社
WALTER DE GRUYTER GMBH
DOI: 10.1351/PAC-CON-12-09-03
关键词
alkaloid synthesis; bioactive molecules; cycloadditions; drug discovery; heterocyclic chemistry; organic chemistry
资金
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [0910560] Funding Source: National Science Foundation
Intramolecular cycloadditions of bicyclo[1.1.0]butylalkyl-amines represent a rich source of novel heterocyclic scaffolds. As a function of the side chain attached to the amine, formal ene- or [2 + 2] cycloaddition products can be obtained in moderate to high yields. By suitable further functionalizations, a library of 3-azatricyclo[5.1.1.0(1,5)]-nonanes was prepared and interrogated in 450 biological assays. This discovery collection was found to generate high hit rates and yet the individual samples demonstrated sufficient selectivity to fulfill robust lead criteria. These applications of bicyclo[1.1.0]butanes demonstrate that new synthetic chemistry and novel architectures are promising starting points for the generation of high-value discovery libraries.
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