ChemInform Abstract: Convenient and Scalable Process for the Preparation of Bupropion Hydrochloride via Efficient Bromination of m‐Chloropropiophenone with N‐Bromosuccinimide.

Abstract

Convenient and Scalable Process for the Preparation of Bupropion Hydrochloride via Efficient Bromination of m-Chloropropiophenone with N-Bromosuccinimide.-A convenient, scalable, and commercially viable process for the production of the antidepressant drug bupropion hydrochloride (III) is reported. The process relies upon an improved large-scale synthesis of key intermediate (II) via NBS bromination. The improved methodology provides the desired product in good overall yield and at considerably lower cost than existing processes. -(REDDY, Y. T.; REDDY, P. N.; REDDY, M. N.; RAJITHA, B.; CROOKS*, P. A.; Synth. Commun. 40 (2010) 11, 1566-1573,

Efficient One‐Pot Syntheses of 7‐Alkyl‐6H,7H‐naphtho[1,2:5,6]pyrano‐[3,2‐c]chromen‐6‐ones by 1‐Methyl‐3‐(2‐(sulfooxy)ethyl)‐1H‐imidazol‐3‐ium Chloride

“…Chromenes constitute a major class of naturally occurring compounds , and interest in their chemistry continues unabated because of their wide range of biological and therapeutic properties such as antioxidant , antibacterial , cytotoxic , anticancer , and antihypertensive activity . Considering the aforementioned reports, development of new and simple synthetic methods for efficient preparation of new chromenes is an interesting challenge.…”

Biginelli and Hantzsch-Type Reactions Leading to Highly Functionalized Dihydropyrimidinone, Thiocoumarin, and Pyridopyrimidinone Frameworks via Ring Annulation with β-Oxodithioesters

“…In the 1970s and 1980s, interest slowly increased, and the scope of the original cyclocondensation reaction shown in Scheme was gradually extended by variation of all the three building blocks allowing access to a large number of attractive multifunctionalized DHPMs. A plethora of useful methodologies involving various types of homogeneous and heterogeneous catalysts , have been elaborated in order to keep the simplicity and to improve the efficiency of the classical Biginelli protocol and to simultaneously overcome its undesirable features. Asymmetric and chemo/regioselective synthesis of Biginelli products using organocatalysts have been developed.…”