摘要 |
PURPOSE:To obtain the subject compound useful as a medicine as an osteogenesis promoter by reacting an exo-methylene derivative with an ene-yne derivative. CONSTITUTION:A compound of formula I [R<1> is H, a tri(1-7C hydrocarbon)silyl, a 2-7C acyl or a group to form an acetal bond with 0 of OH; X is Br, I or trifluoromethanesulfonyl] with a compound of formula II [R<2> and R<3> are each H or a tri(1-7C hydrocarbon)silyl, a 2-7C acyl or a group to form an acetal bond with 0 of OH] in the presence of a palladium catalyst (e.g. tris(dibenzylideneacetone)palladium chloroform-triphenylphosphine to give a vitamin D3 lactone derivative of formula III. The compound of formula III is optionally deprotected to give a vitamin D3 lactone derivative of formula IV. |