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早于三十年代初,就从黄体分离得天然孕激素孕酮(1_a,R=CH_3,R′=H)的纯品,并证明它具有抑制排卵作用,但由于17-侧链易于代谢降解而口服无效。至三十年代末,在发现17α-烷基睾丸素的口服孕激素活性之后,筛选出第一个口服孕激素乙炔睾丸素(2_a,R=R′=CH_3)。嗣后,合成避孕药的研究日益发展。以1_a为母体,在其代谢位置(17 α,16 α,11 β,6 α等)引入基团以抑制化合物的体内代谢,又可增加化合物的口服孕激素活性。例如,17 α-乙酰氧基孕酮(1b,R=CH_3,R′=OAc)和己酸孕酮[1_c,R=CH_3,R′=OCO(CH2)_4CH_3]均为口服有效的孕激素。以2a 为母体,通过增减甲基、引入
As early as the early 1930s, a pure product of progesterone progesterone (1-a, R = CH 3, R ’= H) was isolated from the corpus luteum and proved to have an inhibitory effect on ovulation, but since the 17-side chain is readily metabolically degraded Oral invalid. By the late 1930s, the first oral progestin acetylene testosterone (2-a, R = R ’= CH_3) was screened after the oral progestin activity of 17α-alkyl testosterone was found. Subsequently, the development of synthetic contraceptives is growing. With 1-a as the parent, the introduction of a group at its metabolic site (17 α, 16 α, 11 β, 6 α, etc.) inhibits the in vivo metabolism of the compound and increases the oral progestin activity of the compound. For example, 17α-acetoxyprogesterone (1b, R = CH_3, R ’= OAc) and caproperacetic acid [1_c, R = CH_3, R’ = OCO (CH2) _4CH_3] are all orally available progestins. To 2a as the parent, through the increase and decrease of methyl, introduced