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JOURNAL ARTICLE
RESEARCH SUPPORT, NON-U.S. GOV'T
Skeletal Diversity in Combinatorial Fashion: A New Format for the Castagnoli-Cushman Reaction.
ACS Combinatorial Science 2017 November 14
A new format for the Castagnoli-Cushman reaction of structurally diverse dicarboxylic acids, amines, and aldehydes in the presence of acetic anhydride as dehydrating agent is described. The reaction is distinctly amenable to parallel format: the combinatorial array of 180 reactions delivered 157 products of >85% purity without chromatographic purification (of this number, 143 compounds had >94% purity). The new method offers a convenient preparation of the skeletally and peripherally diverse, lead- and druglike γ- and δ-lactam carboxylic acids with high diastereoselectivity in combinatorial fashion.
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