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A Practical Method for the Large-Scale Preparation of the P‑Chiral Dihydrobenzoazaphosphole Core by Chemical Resolution

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journal contribution
posted on 05.08.2022, 22:20 authored by Jean-Nicolas Desrosiers, Yibo Xu, Stephanie C. Kosnik, Bo Qu, Kendricks S. Lao, Chris H. Senanayake, Yongda Zhang
pivZPhos, as an effective ligand in the Cu-catalyzed asymmetric hydrogenation of ketones and aminoboration of alkenes, is prepared efficiently from the corresponding triflate of P-chiral dihydrobenzoazaphosphole 1. However, the previous approach to 1 by chiral separation is time-consuming and costly, preventing its production and further application on a large scale. In this report, a practical method for the large-scale preparation of 1 was developed via chiral chemical resolution with (1S,2S)-diaminocyclohexane as an effective resolution reagent.