Weier R M, Hofmann L M
J Med Chem. 1975 Aug;18(8):817-21. doi: 10.1021/jm00242a011.
A variety of esters of 17-hydroxy-3-oxo-17alpha-pregn-4-ene-7alpha,21-dicarboxylic acid-gamma-lactone (7a) was synthetized in a sequence using the corresponding 3-oxo-4,6-diene (2) as starting material. The methyl (5), ethyl (7c), and isopropyl (7e) esters as well as the C-1 unsaturated methyl ester (8a) showed good oral and subcutaneous activity (MED less than or equal to 0.41 mg). Some general observations on structure-activity relationships are made.
以相应的3-氧代-4,6-二烯（2）为起始原料，通过一系列反应合成了多种17-羟基-3-氧代-17α-孕甾-4-烯-7α,21-二羧酸-γ-内酯（7a）的酯。甲酯（5）、乙酯（7c）、异丙酯（7e）以及C-1不饱和甲酯（8a）均显示出良好的口服和皮下活性（最小有效剂量小于或等于0.41毫克）。对构效关系进行了一些一般性观察。
