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1.发明公开PALLADIUM CATALYZED ALKYLATIVE CYCLIZATION USEFUL IN SYNTHESIS OF VITAMIN D AND ANALOGUES. 失效钯催化的烷基化环化使用含维生素D及其类似物的合成适用于您。
公开(公告)号：EP0630361A4
公开(公告)日：1995-08-23
申请号：EP93904940
申请日：1993-02-05
发明人： TROST BARRY M , DUMAS JACQUES
IPC分类号： B01J31/18 , B01J31/24 , C07B37/04 , C07B37/10 , C07B61/00 , C07C2/86 , C07C13/465 , C07C17/26 , C07C17/272 , C07C22/00 , C07C23/18 , C07C29/44 , C07C33/44 , C07C35/21 , C07C41/30 , C07C43/178 , C07C401/00 , C07F7/18 , C07C13/36 , C07C13/38 , C07C403/00 , C07C403/02
CPC分类号： C07F7/1892 , C07B37/10 , C07C17/2635 , C07C22/00 , C07C33/44 , C07C35/21 , C07C401/00 , Y02P20/55
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.
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2.发明公开PALLADIUM CATALYZED ALKYLATIVE CYCLIZATION USEFUL IN SYNTHESES OF VITAMIN D AND ANALOGUES 失效钯催化的烷基化环化合成维生素D及其衍生物的
公开(公告)号：EP0738251A4
公开(公告)日：1997-05-14
申请号：EP95906663
申请日：1994-12-19
发明人： TROST BARRY M , DUMAS JACQUES
IPC分类号： B01J31/24 , C07B37/10 , C07C17/26 , C07C22/00 , C07C401/00 , C07C13/36 , C07C13/38 , C07C403/00
CPC分类号： C07C401/00 , C07B37/10 , C07C17/2635 , C07C22/00 , Y02P20/55
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.
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