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Describes the synthesis of the penultimate intermediate in an mTOR inhibitor, indicating a novel synthetic route.
The route and process for the penultimate intermediate toward an mTOR inhibitor GSK332 in GSK’s respiratory portfolio is described. It relies on a heterocycle formation from a crystalline sodium ketoester enolate and an amidine derived from Pd-catalyzed cyanation of an azaindole. The final step involves an S N Ar reaction through selective activation by a hindered sulfonyl chloride and Lewis acid activation to accelerate the rate.
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Barcan et al. (2026) studied this question.
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