钯催化硼酸对芳基卤化物的羟基化反应。

Palladium-Catalyzed Hydroxylation of Aryl Halides with Boric Acid.

机构信息

CAS Key Laboratory of Synthetic and Self-Assembly Chemistry for Organic Functional Molecules, Center for Excellence in Molecular Synthesis, University of Chinese Academy of Sciences, Shanghai Institute of Organic Chemistry, 345 Lingling Road, Shanghai 200032, China.

出版信息

Org Lett. 2020 Nov 6;22(21):8470-8474. doi: 10.1021/acs.orglett.0c03069. Epub 2020 Oct 21.

DOI:10.1021/acs.orglett.0c03069

PMID:33086009

Abstract

Boric acid, B(OH), is proved to be an efficient hydroxide reagent in converting (hetero)aryl halides to the corresponding phenols with a Pd catalyst under mild conditions. Various phenol products were obtained in good to excellent yields. This transformation tolerates a broad range of functional groups and molecules, including base-sensitive substituents and complicated pharmaceutical (hetero)aryl halide molecules.

摘要

硼酸（B(OH)）在 Pd 催化剂作用下，被证明是一种高效的氢氧根试剂，可在温和条件下将（杂）芳基卤化物转化为相应的酚类化合物。各种酚类产物的产率均为良好至优秀。这种转化可耐受广泛的官能团和分子，包括对碱敏感的取代基和复杂的药物（杂）芳基卤化物分子。