Department of Pharmaceutical Sciences and Chemistry, University of Pittsburgh, 3501 Fifth Avenue, BST1 11019, Pittsburgh, PA 1526, USA.
Chem Biol Drug Des. 2010 Mar;75(3):277-83. doi: 10.1111/j.1747-0285.2009.00942.x. Epub 2010 Jan 19.
The design of an unprecedented multicomponent reaction to and synthesis of 2-amino-5-ketoaryl pyrroles are described. The compounds (14 examples) can be synthesized by reacting aminoacetophenone sulfonamides, (hetero)aromatic aldehydes, and malonodinitrile or cyanoacetic acid derivatives in one-pot manner. Pharmacophore features and potential applications of this new scaffold are discussed.
描述了一种前所未有的多组分反应和 2-氨基-5-芳基吡咯的合成设计。这些化合物(14 个实例)可以通过在一锅反应中使氨基苯乙酮磺酰胺、(杂)芳族醛和丙二腈或氰基乙酸衍生物反应来合成。讨论了这个新支架的药效团特征和潜在应用。