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

piv ZPhos, 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 (1 S ,2 S )-diaminocyclohexane as an effective resolution reagent.