13α-取代-去-C-环-19-去亚甲基-1α,25-二羟基维生素D3类似物的合成

Synthesis of 13α-Substituted-des-C-ring-19-nor-1α,25-dihydroxyvitamin D_3 Analogs

以维生素D3为起始原料,经臭氧化,Baeyer-Villiger氧化内酯化,开裂六元环,二氧化钌(RuO2)引进C-25位羟基,最后经Horner-Wittig反应偶合D环和A环得到13-取代-去-C-环-19-去亚甲基-1α,25-二羟基维生素D3类似物(12a,12b).

The syntheses of 13α-substituted-des-C-ring-19-nor-1α,25-dihydroxyvitamin D3 analogs (12a, 12b) are described. The sequence involves using vitamin D3 as a starting material, cleavage of the six-member ring by Baeyer Villiger reaction, introducing the C-25-hydroxy group by ruthenium oxide, and coupling the D-ring and A-ring by Horner-Witting reaction.