A metal-free, mild and efficient method for the synthesis of thiazolo[3,2-a]indoles has been developed starting from indoline-2-thiones. The reaction methodology involves first the formation of thermally labile 2-(prop-2-ynylthio)-1H-indole intermediates, which undergo base-mediated intramolecular hydroamination to produce the title compounds in excellent yields.

One-pot synthesis of [1,3]thiazino[3,2-a]indol-4-one frameworks is developed in aqueous medium and the anti-proliferative activity of the synthesized compounds is evaluated against two triple negative breast cancer cell lines.

A one‐pot, atom‐economical multicomponent reaction of 2‐bromoindole‐3‐carbaldehydes, alkynes and ammonia was developed in the presence of copper catalyst for the synthesis of a series of 3‐aryl‐γ−carboline derivatives in good to high yields. The developed reaction involved formation of imine followed by copper‐catalyzed directed Sonogashira coupling and intramolecular hydroamination sequence of reactions. This multicomponent approach features mild reaction conditions and good functional group tolerance to access variety of 3‐aryl γ‐carbolines.