论文部分内容阅读
自从1954年Fried和Sabo报告了第一个含氟甾体激素——9α-氟皮貭醇(9α-fluorohydrocortisone,I_α)的合成以后,近十年来对于含氟甾体激素的研究非常热烈,因为在皮貭醇(I_b)分子的C_9-位置引入一个α-氟原子以后,它的抗炎功效比其母体增加了十多倍,鈉的保留作用亦增強。由于氟原子在甾体分子中对生理作用具有显著影响,因此引起了許多甾体工作者的注意,大家紛紛研究甾体环核中各个位置上引入氟原子后对生理作用的改变。經过最近几年来的研究,现在已获得了一系列优良的含氟甾体激素药物,并且通过各种含氟甾体激素的合成,使得含氟的甾体化学得到了发展。本文拟将最近十年来关于在甾体环核中引入氟原子的各种方法作一簡略介紹。欲在甾体环核的某一位置引入一个或数个氟原子时,通常利用甾体分子中在該位置上的某一官能团与适当的氟化試剂作用而得。迄今文献上所报告的用于引入甾核氟原子
Since the first report of the synthesis of 9α-fluorohydrocortisone (I_α) by Fried and Sabo in 1954, the study of steroid-containing steroids has been very intense in the recent decade because After introduction of an alpha-fluorine atom at the C_9-position of the I_b molecule, its anti-inflammatory efficacy has increased by more than 10-fold over its parent and sodium retention has been enhanced. Since fluorine atoms have a significant influence on physiological functions in steroid molecules, many steroid workers have drawn their attention. Many people have studied the physiological effects of introducing fluorine atoms at various positions in the steroid nucleus. After several years of research, a series of excellent steroid hormone drugs have now been obtained and fluorinated steroid chemistry has been developed through the synthesis of various steroid-containing steroids. This article intends to make a brief introduction of various methods for introducing fluorine atoms into the nucleus of steroid nucleus in the recent ten years. The introduction of one or several fluorine atoms at a position in the nucleus of a steroid nucleus usually results from the interaction of a functional group in the steroid molecule at that position with a suitable fluorinating reagent. So far reported in the literature for the introduction of steroidal fluorine atoms