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Solid-phase Synthesis of [4.4] Spirocyclic Oximes
Published on: February 6, 2019
Development of a One-Step Synthesis of oxa-Spirocyclic Diphosphine Ligands Driven by Their Application in the
Gen-Qiang Chen1,2, Renwei Xiao1, Xiaobing Ding1
1Medi-X Pingshan and Department of Chemistry, Southern University of Science and Technology, Shenzhen 518000, People's Republic of China.
Abstract:
Herein we have developed a highly practical and efficient one-step coupling protocol for the synthesis of chiral spiro diphosphine ligands, especially for the oxa-spiro diphosphine ligands O-SDP, which showed excellent reactivity and diastereoselectivity in the asymmetric hydrogenation of a key intermediate of Sacubitril. It should be noted that the one-step coupling protocol could be operated on a kilogram scale, and the resulting ruthenium catalyst of O-SDP could hydrogenate the key intermediate of Sacubitril on an industrial scale.
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