Abstract

Asymmetric synthesis of P‐stereogenic phosphonates presents a great challenge. Following this target we disclose herein a DKR strategy towards the O–P coupling reaction between an easily accessible enantiopure phenol bearing a chiral sulfinyl auxiliary and a commercially available or easily accessible racemic H‐phosphinate. Although moderate to high chiral induction is achieved, several diastereopure phosphonates can be afforded either by crystallization or flash chromatography. Thus accessed optically pure P‐stereogenic precursors may be used as appealing building blocks to rapidly assembly original privileged scaffolds as illustrated via the synthesis of a chiral ligand such as PAMPO.

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