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Abstract
The beta-ketoester 1 is one of the critical starting materials used in the second-generation synthesis of adagrasib. Disclosed within is a new, streamlined, operationally simple and more environmentally friendly three-step telescoped protocol which was demonstrated on a >100 kg batch with an overall yield of 70%. Identification of the shortcomings and the quality issues of the initial route are discussed. The process development work overcoming these challenges and leading to the new route of synthesis is described.
Supplementary materials
Title
Additional experiments and NMR spectra
Description
General experimental details, experiments with formaldehyde, reprocessing experiments, inorganic base screening, X-Ray data, characterization data and NMR spectra.
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