Enantioselective synthesis of (−)-(R) Silodosin by ultrasound-assisted diastereomeric crystallization

Synthesis of Silodosin by Copper‐Catalysed C–C Arylation

“…It acts as a selective α 1A adrenergic receptor antagonist, and is currently used for the treatment of LUTS (lower urinary tract symptoms) [1] and dysuria associated with benign prostatic hyperplasia (BPH). [3][4][5] The strategy diclosed in the initial patent, [1] which was improved by Sun et al, [3] needs 19 synthetic steps to obtain enantiopure silodosin; it uses toxic cyanides, and a low-yielding resolution. [2] The first marketing authorisation of silodosin was granted to Kissei in Japan in 2006; two years later, they obtained the FDA authorisation for commercialisation of silodosin in the USA.…”