Diverse Strategies for the Synthesis of the Indoline Scaffold

Because indoline is an important intermediate of angiotensin‐converting enzyme (ACE) inhibitor and the antihypertensive drug “pentopril”, and also because it is a ubiquitous scaffold found in the structures of several naturally bioactive alkaloids such as vinblastine, strychnine, (–)‐physostigmine, ajmaline, and (+)‐aspidospermidine, the synthesis of this “privileged structure” is meaningful in the design of new biologically active medicines. This microreview describes the recent advances in the synthesis of indoline derivatives, including Cu‐ and Pd‐catalyzed reactions, metal‐free approaches (radical reaction), as well as other types of reactions.