Clickable transformation of nitriles (RCN) to oxazolyl sulfonyl fluoride warheads
The protocol for simple, efficient, and mild synthesis of oxazolyl sulfonyl fluorides was developed through Rh2(OAc)4-catalyzed annulation of methyl-2-diazo-2-(fluorosulfonyl)acetate (MDF) or its ethyl ester derivative with nitriles. This practical method provides a general and direct route to a unique class of highly functionalized oxazolyl-decorated sulfonyl fluoride warheads with great potential in medicinal chemistry, chemical biology, and drug discovery.
Preparation of sodium sulfonates using by copper as catalyst
The sodium alkyl sulfonates were prepared by Strecker reaction. The synthesis of sodium chloroethyl sulfonate from dichloroethane and sodium sulfite with different catalysts, it was found that copper was an efficient catalyst with a yield (81%). The reaction conditions were also optimized to make the route more competitive and suitable for large-scale industrial production. Besides, some more sulfonates were also obtained with copper as catalyst via Strecker reaction.