Synthesis of Side-Chain Locked Analogs of 1α,25-Dihydroxyvitamin D3 Bearing a C17 Methyl Group

Org Lett. 2018 May 4;20(9):2641-2644. doi: 10.1021/acs.orglett.8b00849. Epub 2018 Apr 13.

Abstract

A convergent synthesis of side-chain locked vitamin D analogs 3 and 4, which bind strongly in silico to the vitamin D receptor (VDR), is described. The synthetic approach features an SN2'- syn displacement of carbamates by cuprates to set the challenging quaternary stereogenic center at C17 and a Pd-catalyzed construction of the triene system in the presence of a diyne moiety.

Publication types

  • Research Support, Non-U.S. Gov't