论文部分内容阅读
吲哚-2-甲酸和(S)-吲哚啉-2-甲酸均是具有生物活性的天然产物和众多降压药的特征结构片段,报道了它们的合成及其相互转化研究进展.吲哚啉-2-甲酸可由吲哚-2-甲酸还原制得,其中(S)-吲哚啉-2-甲酸可由外消旋体拆分或通过不对称合成法制备,其中“手性源法”作为一种新出现的方法具有较好的前景.吲哚-2-甲酸可由Fischer吲哚合成法制备,或通过取代苯胺或苯甲醛制备,也可通过吲哚啉衍生物氧化脱氢制备,其中Fischer合成法仍具有较强的竞争力.
Indole-2-carboxylic acid and (S) -indoline-2-carboxylic acid are both biologically active natural products and many antihypertensive drugs. The progress of their synthesis and their interconversion has been reported. 2-carboxylic acid can be prepared from indole-2-carboxylic acid by reduction, wherein (S) -indoline-2-carboxylic acid can be resolved by racemate or by asymmetric synthesis, where “ ”As a new emerging method has a good prospect.indole-2-carboxylic acid can be prepared by Fischer indole synthesis, or by substituting aniline or benzaldehyde can also be prepared by oxidative dehydrogenation of indoline derivatives , Of which Fischer synthesis method still has a strong competitive edge.