Syntheses of Indole-2-carboxylic Acid and Indoline-2-carboxylic Acid and Transformation from Each Other

Abstract

Indole-2-carboxylic acid and indoline-2-carboxylic acid are common building block in natural products with bioactivities and anti-hypertension pharmaceuticals. The syntheses and transformation from each other were reviewed. Indoline-2-carboxylic acid can be got from the reduction of indole-2-carboxylic acid and the S enantiomer can be achieved from the resolution of the racemic mixture with chemical reagents or enzymes. The chiral pool synthesis, emerged recently, will play an important role in the future. In-dole-2-carboxylic acid can be formed from Fischer way or substituted anilines and benzaldehydes.

Key words: indole-2-carboxylic acid, indoline-2-carboxylic acid, transformation, progress

CLC Number:

O626

Cite this article

LIU Jin-Qiang, QIAN Chao, CHEN Xin-Zhi. Syntheses of Indole-2-carboxylic Acid and Indoline-2-carboxylic Acid and Transformation from Each Other[J]. Chin. J. Org. Chem., 2011, 31(05): 634-645.

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