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