The synthesis of silodosin, an antidysuria drug, has been accomplished starting from commercially available indoline. The synthetic strategy is based on Cu<sup>I</sup>-catalysed C-C arylation, regioselective cyanation, and diastereoselective reductive amination. The enantiopure compound was obtained by selective crystallisation of a diasteroisomeric mixture.
Synthesis of silodosin by copper-catalysed C-C arylation / F. Calogero, P. Allegrini, E. Attolino, D. Passarella. - In: EUROPEAN JOURNAL OF ORGANIC CHEMISTRY. - ISSN 1434-193X. - 2015:27(2015), pp. 6011-6016. [10.1002/ejoc.201500753]
Synthesis of silodosin by copper-catalysed C-C arylation
F. Calogero
;D. PassarellaUltimo
2015
Abstract
The synthesis of silodosin, an antidysuria drug, has been accomplished starting from commercially available indoline. The synthetic strategy is based on CuI-catalysed C-C arylation, regioselective cyanation, and diastereoselective reductive amination. The enantiopure compound was obtained by selective crystallisation of a diasteroisomeric mixture.
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