Tetrahedron letters

Mild and convenient N-formylation protocol in water-containing solvents

BA Aleiwi, K Mitachi, M Kurosu

文献索引：Aleiwi, Bilal A.; Mitachi, Katsuhiko; Kurosu, Michio Tetrahedron Letters, 2013 , vol. 54, # 16 p. 2077 - 2081

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被引用次数: 13

摘要

We have realized that N-formylations of free amines of some drug leads can improve PK/PD property of parent molecules without decreasing their biological activities. In order to selectively formylate primary amines of polyfunctional molecules, we have sought a mild and convenient formylation reaction. In our screening of N-formylation of an α-amino acid, l- phenylalanine, none of formylation conditions reported to date yielded the desired HCO-l- ...