SYNTHESIS OF 1 alpha,25-DIHYDROXY-2 beta-(3-HYDROXYPROPOXY)VITAMIN D-3 (ELDECALCITOL) AND RELATED COMPOUNDS BY THE TROST CONVERGENT METHODOLOGY

[摘要]：Using Trost convergent methodology, the synthesis of 1 alpha,25-dihydroxy-2 beta-(3-hydroxypropoxy)vitamin D-3 (eldecalcitol) for the improved and industrial scale production and related putative metabolites of eldecalcitol is summarized. In addition, A-ring diastereomers at the 1- and 3-positions of eldecalcitol are described. The synthesis centers on a key palladium-catalyzed alkylative cyclization and coupling of ene-ynes that constitute the A-ring fragment to bromomethylenes comprising the C/D-ring fragment which affords the requisite triene framework of vitamin D-3 analogs.

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