Skeletal Diversity in Combinatorial Fashion: A New Format for the Castagnoli–Cushman Reaction,ACS Combinatorial Science

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Skeletal Diversity in Combinatorial Fashion: A New Format for the Castagnoli–Cushman Reaction
ACS Combinatorial Science Pub Date : 2017-10-26 00:00:00 , DOI: 10.1021/acscombsci.7b00118
Anastasia Lepikhina ₁ , Dmitry Dar’in ₁ , Olga Bakulina ₁ , Evgeny Chupakhin ₂ , Mikhail Krasavin _{1,

2}

Affiliation

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.

中文翻译：

组合方式的骨骼多样性：Castagnoli-Cushman反应的新形式

描述了在乙酸酐作为脱水剂存在下，结构多样的二元羧酸，胺和醛的Castagnoli-Cushman反应的新形式。该反应明显适合于平行反应：180个反应的组合阵列无需色谱纯化即可提供157种纯度> 85％的产物（其中143种化合物的纯度> 94％）。该新方法以组合的方式提供了方便的制备具有高非对映选择性的骨架和外围变化的铅和药物样γ-和δ-内酰胺羧酸。

更新日期：2017-10-26

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