Abstract

Herein, the development of an efficient and practical, glycerol promoted, green and sustainable synthesis of diversified aryloxy propanolamines, including propranolol and atenolol, which are among the most prescribed drugs globally, is reported. The salient feature of this protocol is the use of glycerol, a bio-renewable, eco-friendly bioorganic molecule, as a recyclable solvent cum promoter for effecting the reaction. The other key features of this method are the use of mild reaction conditions, broad substrate scope, short reaction times, good to excellent yields, high atom economy and column-free purification. An asymmetric version of the protocol was also successfully demonstrated, allowing access to the R and S isomers of propranolol. The protocol was successfully scaled up to multi-gram scale, highlighting the robustness and practicability of the current method, making it an attractive, eco-friendly alternative to methods currently employed for obtaining propranolol, atenolol and other related medicinally significant aryloxy propanolamines.

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