Tetrahedron Letters

A novel approach for the synthesis of Crizotinib through the key chiral alcohol intermediate by asymmetric hydrogenation using highly active Ir-Spiro-PAP catalyst

JQ Qian, PC Yan, DQ Che, QL Zhou, YQ Li

Index: Qian, Jian-Qiang; Yan, Pu-Cha; Che, Da-Qing; Zhou, Qi-Lin; Li, Yuan-Qiang Tetrahedron Letters, 2014 , vol. 55, # 9 p. 1528 - 1531

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Citation Number: 2

Abstract

Abstract A novel approach for the synthesis of Crizotinib (1) is described. In addition, new efficient procedures have been developed for the preparation of (S)-1-(2, 6-dichloro-3- fluorophenyl) ethanol (2) and tert-butyl 4-(4-(4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborolan-2-yl)- 1H-pyrazol-1-yl) piperidine-1-carboxylate (4), the key intermediates required for the synthesis of Crizotinib.