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    • 2. 发明申请
    • Processes for preparation of 9,11-epoxy steroids and intermediates useful therein
    • 制备9,11-环氧类固醇及其中有用的中间体的方法
    • US20030055274A1
    • 2003-03-20
    • US10112355
    • 2002-03-29
    • G.D. Searle & Company
    • John S. NgChin LiuDennis K. AndersonJon P. LawsonJoseph WieczorekSastry A. KundaLeo J. LetendreMark J. PozzoYuen-Lung L. SingPing T. WangEdward E. YonanRichard M. WeierThomas B. KowarJulio A. BaezBernhard Erb
    • C07J001/00
    • C12P33/10C07D301/12C07J1/0059C07J21/00C07J21/003C07J31/006C07J41/0094C07J53/002C07J71/0005C07J71/0015C12P33/005
    • Multiple novel reaction schemes, novel process steps and novel intermediates are provided for the synthesis of epoxymexrenone and other compounds of formula (I) wherein: nullAnullAnull represents the group nullCHR4nullCHR5null or nullCR4nullCR5null, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl, lower alkoxy, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, cyano, aryloxy; R1 represents an alpha-oriented lower alkoxycarbonyl or hydroxyalkyl radical; nullBnullBnull represents the group nullCHR6nullCHR7null or an alpha- or beta-oriented group (III), where R6 and R7 are independently selected from the group consisting of hydrogen, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy; and R8 and R9 are independently selected from the group consisting of hydrogen, hydroxy, halo, lower alkoxy, acyl, hydroxyalkyl, alkoxyalkyl, hydroxycarbonyl, alkyl, alkoxycarbonyl, acyloxyalkyl, cyano and aryloxy, or R8 and R9 together comprise a carbocyclic or heterocyclic ring structure, or R8 or R9 together with R6 or R7 comprise a carbocyclic or heterocyclic ring structure fused to the pentacyclic D ring. 1
    • 提供了多种新的反应方案,新的工艺步骤和新的中间体,用于合成环氧麦芽糖酮和式(I)的其它化合物,其中:-AA-表示-CHR 4 -CHR 5 - 或-CR 4 = CR 5 - ,R 3,R 4和 R5独立地选自氢,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,芳氧基; R1表示α-取代的低级烷氧基羰基或羟烷基; -BB-表示基团-CHR6-CHR7-或α取代或β-取代基团(III),其中R6和R7独立地选自氢,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; 并且R 8和R 9独立地选自氢,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,或者R 8和R 9一起包含碳环或杂环 结构或R8或R9与R6或R7一起包含与五环D环稠合的碳环或杂环结构。