Abstract

A new synthesis of lumateperone tosylate is presented based on a novel, efficient method for the resolution of a key intermediate. In order to assure the production of a drug substance of high quality and the recovery of the resolving agent, the diastereomeric salt obtained in the chiral resolution process is transformed to the corresponding dihydrochloride salt. The latter serves as a direct precursor to the one-pot synthesis of lumateperone tosylate salt.

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