Document Report Card

Basic Information

ID: ALA1130618

Journal: Bioorg Med Chem Lett

Title: A novel and practical route to A-ring enyne synthon for 1 alpha,25-dihydroxyvitamin D3 analogs: synthesis of A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D2 and 3-methyl-1,25-dihydroxyvitamin D3.

Authors: Konno K, Maki S, Fujishima T, Liu Z, Miura D, Chokki M, Takayama H.

Abstract: A novel and practical route to the A-ring enyne synthon (2), which can be versatile for a variety of A-ring analogs of 1 alpha,25-dihydroxyvitamin D3 (1), was developed. This novel method led to an improved synthesis of the A-ring diastereomers of 1, the compounds 13-15, and synthesis of the new analogs, 2-methyl-1,25-dihydroxyvitamin D3 (4) with its all possible diastereomers. The biological evaluation of the 2-methyl analogs showed the alpha alpha beta-isomer to be more potent than 1.

CiteXplore: 9871644

DOI: 10.1016/s0960-894x(97)10204-9