Demonstrates a practical synthetic route for KRAS inhibitor building block, indicating scalable production for drug development.
A practical, concise, and scalable synthetic route has been developed for the KRAS inhibitor building block 4-bromo-6-chloro-5-iodo-1-(tetrahydro-2 H -pyran-2-yl)-1 H -indazole. The route comprises six steps, four of which are telescoped, and requires no column chromatography purification. This optimized process has been successfully implemented for the large-scale production of building block 1 at up to ∼200 kg with an overall yield of 61.68%.
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Zhu et al. (2026) studied this question.
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