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    • 5. 发明公开
    • A process for producing an alpha-acyloxy-alpha beta-unsaturated carbonyl compound and a 20-acyl-oxy-17(20)-methylen-21-al-steroid compound
    • 一种用于制备α-酰氧基α-β-不饱和化合物和20-酰氧基-17(20) - 亚甲基-21-人 - 甾类衍生物的过程。
    • EP0306969A2
    • 1989-03-15
    • EP88114770.6
    • 1988-09-09
    • NIPPON ZEON CO., LTD.
    • Watanbe, KiyoshiKataoka, HideakiGoto, Kuniaki
    • C07J13/00C07C69/24C07C69/145C07C67/30C07J75/00
    • C07J75/00C07C67/313C07J1/0048C07J13/005C07J13/007
    • There are disclosed a process for producing an α-acyloxy-α,β-unsaturated carbonyl compound represented by the general formula (VI):
      wherein Ri, R 2 and R4 are independently hydrogen atoms or substituted or unsubstituted hydrocarbon residues, or Ri, R 2 and R 4 , when taken together with one another in an optional combination, form a ring, R 3 is a substituted or unsubstituted hydrocarbon residue, and indicates that the configuration may be either E-configuration or Z-configuration, in particular, a 20-acyloxy-17(20)-methylen-21-al-steroid represented by the partial structural formula (II):
      wherein R is a hydrocarbon residue, and indicates that the configuration of the acyloxy group and the formyl group bonded to the carbon atom at the 20-position may be either E-configuration or Z-configuration, which comprises oxidizing a propargyl ester represented by the general formula (V):
      wherein Ri, R 2 , R 3 and R 4 have the same meanings as defined above; an al-steroid compound having the above partial structural formula which is an intermediate for producing a 21-acyloxy-20-keto-delta16-steroid being extremely useful as an intermediate for important corticoids as drugs and obtained by being subjected said al-steroid to isomerization reaction; and a process for producing a 21-acyloxy-20-keto- delta 16 -steroid which comprises oxidation reaction and isomerization reaction.
    • 有游离缺失盘的处理在阿尔法酰氧基-α,由通式(VI)表示β-不饱和羰基化合物制备: worin R1,R2和R4为氢原子或unabhängigsubstituiertem奥德unsubstituiertem烃残基,或R1 ,R2和R4,当与在和任意组合彼此结合在一起形成一个环,R 3是一个substituiertem奥德unsubstituiertem烃残基,@@@表示DASS模具结构可以是E构型或Z构型,特别是 ,20酰氧基 - 17(20)亚甲基 - 21-AL-​​类固醇由部分结构式(II)表示: worin R是烃残基,并且表示@@@做的酰氧基的构 和在20位键合到碳原子上的甲酰基可以是E构型或Z构型,该方法包括氧化由通式(V)表示的炔丙基酯: worin R1,R2,R3和 R4具有相同的含义如上所定义; 到人类固醇化合物,其具有的所有这些是用于制造21 - 酰氧基-20-酮基 - 德尔塔中间上述部分结构式<1> <6>类固醇是作为中间体用于重要肾上腺皮质激素作为药物非常有用的,并通过而获得 进行说人类固醇至异构化反应; 以及一种用于制造21 - 酰氧基-20-酮基 - 德尔塔的处理<1> <6>类固醇,其包括氧化反应和异构化反应。