Asymmetric Synthesis of Methyl N-(tert-Butoxycarbonyl)indoline-2-carboxylates

作者：Zhang, Qianqian; Ding, Qunshan; Song, Chuanjun^*; Chang, Junbiao^*

来源：Chinese Journal of Organic Chemistry, 2018, 38(1): 221-227.

DOI：10.6023/cjoc201708002

• indoline-2-carboxylate
• Williams chiral auxiliary
• Buchwald-Hartig coupling
• asymmetric synthesis

As a characteristic structural motif of numerous biologically active natural products and new drugs, chiral indoline derivatives have attracted much attention of chemists. Although many methods are available, there is still great need to develop a new, simple and highly efficient asymmetric synthetic method of indoline derivatives. Starting from Williams chiral auxiliary, a variety of methyl (R)-N-(tert-butoxycarbonyl) indoline-2-carboxylates were obtained with high overall yields and enantioselectivity through nucleophilic substitution, intramolecular Buchwald-Hartwig coupling reaction, etc.

• 出版日期2018-1-25
• 单位郑州大学