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New synthesis of a late-stage tetracyclic key intermediate of lumateperone.


ABSTRACT: New approaches have been tested for the synthesis of lumateperone intermediates. As a result of these efforts, a novel synthesis of the late-stage tetracyclic key intermediate of lumateperone starting from the commercially available quinoxaline is described. The tetracyclic skeleton was constructed by the reaction of 1-trifluoroacetyl-4-aminoquinoxaline with ethyl 4-oxopiperidine-1-carboxylate in a Fischer indole synthesis. The inexpensive starting material, the efficient synthetic steps, and the avoidance of the borane-based reduction step provide a reasonable potential for scalability.

SUBMITTER: Milen M 

PROVIDER: S-EPMC9194496 | biostudies-literature |

REPOSITORIES: biostudies-literature

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