通过非对映选择性还原柯普重排和官能团转化策略合成1,2,4-三官能团化环己烷
1,2,4-Trifunctionalized Cyclohexane Synthesis via a Diastereoselective Reductive Cope Rearrangement and Functional Group Interconversion Strategy.
作者信息
Mannchen Michael D, Ghiviriga Ion, Abboud Khalil A, Grenning Alexander J
机构信息
Department of Chemistry, University of Florida, Gainesville, Florida 32603, United States.
Center for NMR Spectroscopy, Department of Chemistry, University of Florida, Gainesville, Florida 32603, United States.
出版信息
Org Lett. 2021 Nov 19;23(22):8804-8809. doi: 10.1021/acs.orglett.1c03310. Epub 2021 Nov 1.
Polyfunctionalized cyclohexanes are privileged scaffolds in drug discovery. Reported herein is a method for synthesizing 1,2,4-trifunctionalized cyclohexanes via diastereoselective reductive Cope rearrangement. The scaffolds obtained can be derivatized by orthogonal functional group interconversion to cyclohexanes bearing a 1-amide, 2-branched arylallyl, and variable 4-functional group.
多官能团化环己烷是药物研发中重要的骨架结构。本文报道了一种通过非对映选择性还原Cope重排合成1,2,4-三官能团化环己烷的方法。所得到的骨架结构可通过正交官能团转化衍生为带有1-酰胺基、2-支链芳基烯丙基和可变4-官能团的环己烷。
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