摘要:
An alkylative cycloaddition method is provided that is particularly useful for the synthesis of many of the Vitamin D analogues with differing side chains. Thus, a preferred synthesis is of Vitamin D analogues having a side chain R1 where a substantially geometrically pure first precursor having structure (I), and a second precursor are provided, the second precursor being a 1,7 enyne. These precursors are reacted in the presence of a palladium catalyst to form compounds having structure (II), where R2 is hydrogen, hydroxyl, lower alkoxy, fluorine, or a protecting group, and R3 is hydrogen, hydroxyl, lower alkoxy, fluorine, or a protecting group.
摘要:
A novel ligand having formula (1) structure has proved remarkably successful in the amination of butadiene monoepoxide, which is a potentially desirable substrate for an asymmetric synthesis providing access to each enantiomer of vinylglycinol. This and other ligands described are useful for chiral induction of bond forming reactions with an epoxide substrate.
摘要:
An alkylative cycloaddition method is provided that is particularly useful for the synthesis of many of the Vitamin D analogues with differing side chains. Thus, a preferred synthesis is of Vitamin D analogues having a side chain R1 where a first precursor having the structure (a), with X being a halide or a pseudo halide, and a second precursor are provided, the second precursor being a 1,7 enyne. These precursors are reacted in the presence of a palladium catalyst to form compounds having structure (1), where R2 is hydrogen, hydroxyl, lower alkoxy, fluorine, or a protecting group, and R3 is hydrogen, hydroxyl, lower alkoxy, fluorine, or a protecting group.