Developing new synthetic approaches for the synthesis of nitrogen-containing heterocyclic compounds from readily available starting materials is an important topic in modern organic chemistry. Of special interest for mimicking natural processes is the synthesis of indole-containing systems as indoles are one of the most widely distributed heterocycles in nature. In particular, 3-acylindoles and their derivatives are ubiquitous in natural products, biologically active compounds and pharmaceuticals, expressing diverse benefits such as hypocholesterolemic, analgesic, anti-inflammatory, immunomodulatory, antiemetic, antivirus and anticancer activities. Indoles are also versatile precursors for the synthesis of alkaloids and other related heterocycles. Pravadoline (1) BPR0L075 ( ) Ramosetron (3)