Palladium catalyzed alkylative cyclization useful in...

C - Chemistry – Metallurgy – 07 – C

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C07C 401/00 (2006.01) C07B 37/10 (2006.01) C07C 17/26 (2006.01) C07C 22/00 (2006.01) C07C 33/44 (2006.01) C07C 35/21 (2006.01) C07F 7/08 (2006.01) C07F 7/18 (2006.01)

Patent

CA 2129136

2129136 9316022 PCTABS00025 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.

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