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Palladium/Xu-Phos-catalyzed asymmetric carboamination towards isoxazolidines and pyrrolidines.

ABSTRACT: An efficient palladium-catalyzed enantioselective carboamination reaction of N-Boc-O-homoallyl-hydroxylamines and N-Boc-pent-4-enylamines with aryl or alkenyl bromides was developed, delivering various substituted isoxazolidines and pyrrolidines in good yields with up to 97% ee. The reaction features mild conditions, general substrate scope and scalability. The obtained products can be transformed into chiral 1,3-aminoalcohol derivatives without erosion of chirality. The newly identified Xu-Phos ligand bearing an ortho-OⁱPr group is responsible for the good yield and high enantioselectivity.

SUBMITTER: Wang Y

PROVIDER: S-EPMC8208297 | biostudies-literature |

REPOSITORIES: biostudies-literature

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