Odalasvir
is a selective inhibitor of hepatitis C virus NS5A protein,
a key target for combination therapies. This paper describes the chemical
process development for the synthesis of this active pharmaceutical
ingredient and the improvements that were achieved over the medicinal
chemistry route. Optimization of all of the reaction conditions and
crystallizations resulted in higher throughput and a highly improved
process mass intensity. The process is robust and has been scaled
up to ∼100 kg batches without issues.
The ethene units of the title compound, C32H24S, a possible candidate for Organic Light‐Emitting Devices, are tilted with respect to the thiophene unit by 6.2 (1) and 9.2 (1)°.
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