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    Processes for preparation of 3-keto-7alpha-alkoxycarbonyl-delta-4,5- steroids and intermediates useful therein
    3.
    发明公开
    Processes for preparation of 3-keto-7alpha-alkoxycarbonyl-delta-4,5- steroids and intermediates useful therein 失效
    一种用于3-酮 - 7alpha烷氧羰Delta4,5甾体和其中间体的制备方法

    公开(公告)号：EP1223174A2

    公开(公告)日：2002-07-17

    申请号：EP02007309.4

    申请日：1997-12-11

    申请人： G.D. SEARLE & CO.

    发明人： Ng, John S. ,  Liu, Chin ,  Anderson, Dennis K. ,  Lawson, Jon P. ,  Wieczorek, Joseph ,  Kunda, Sastry A. ,  Letendre, Leo J. ,  Pozzo, Marc J. ,  Sing, Yuen-Lung L. ,  Wang, Ping T. ,  Yonan, Edward E. ,  Weier, Richard M. ,  Kowar, Thomas R. ,  Baez, Julio A. ,  Erb, Bernhard

    IPC分类号： C07J1/00 ,  C07J21/00 ,  C07J41/00 ,  C07J71/00 ,  C12P33/00 ,  C07D301/12 ,  C07J31/00 ,  C07J53/00 ,  C12P33/10

    CPC分类号： C07J53/002 ,  C07D301/12 ,  C07J1/0059 ,  C07J21/00 ,  C07J21/003 ,  C07J31/006 ,  C07J41/0094 ,  C07J71/0005 ,  C07J71/0015 ,  C12P33/005 ,  C12P33/10

    摘要： Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of Formula I
    wherein:

    -A-A- represents the group -CHR 4 -CHR 5 - or -CR 4 =CR 5 - R 3 , R 4 and R 5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, varyloxy;
    R 1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical;
    -B-B- represents the group -CHR 6 -CHR 7 - or an alpha- or beta- oriented group:
    where R 6 and R 7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and
    R 8 and R 9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R 8 and R 9 together comprise a carbocyclic or heterocyclic ring structure, or R 8 or R 9 together with R 6 or R 7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring.

    摘要翻译： 多个新的反应方案中，新颖的工艺步骤和新的中间体提供了用于epoxymexrenone和其它式化合物的合成I worin：-AA- darstellt组-CHR <4> -CHR <5> - 或-CR < 4> = CR <5> - R的<3>，R <4>和R <5>是unabhängig选自氢，卤素，羟基，低级烷基，低级烷氧基，羟基烷基，烷氧基烷基，羟基羰基，氰基， varyloxy; [R <1>α-取向低级烷氧基羰或羟烷基的三个代表; -BB- darstellt组-CHR <6> -CHR <7> - 或α-或β-取向的基团：氢其中R <6>和R <7>unabhängig选自的选择 卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基; 且R <8>和R <9>是unabhängig选自氢，羟基，卤素，低级烷氧基，酰基，羟基烷基，烷氧基烷基，羟基羰基，烷基，烷氧基羰基，酰氧基烷基，氰基和芳氧基中选择的，或R <8> 且R <9>一起构成碳环或杂环结构，或者R <8>或R <9>，其中R <6>或R一起<7>包括融合到五环D形环的碳环或杂环结构。