Tóth I, Szabó L, Bozsár G, Szántay C, Szekeres L, Papp J G
J Med Chem. 1984 Nov;27(11):1411-5. doi: 10.1021/jm00377a006.
The pharmacologically active (methylenedioxy)- and diethoxyepialloberbane keto esters I have been synthesized with use of the readily available keto esters 2 as starting material. By choice of the appropriate reaction sequence both antipodes of keto ester 2a can be employed to provide any enantiomer of the desired raunescinone analogue 1a. Hypotensive, antihypertensive, and central depressant effects of 1a are described. The principle effect observed for 1a was a potent hypotensive and antihypertensive effect of long duration without depression of the central nervous system.
已使用易于获得的酮酯2作为起始原料合成了具有药理活性的（亚甲二氧基）-和二乙氧基表去甲钩吻酮酮酯I。通过选择合适的反应顺序，酮酯2a的两种对映体均可用于提供所需的雷内西酮类似物1a的任何对映体。描述了1a的降压、抗高血压和中枢抑制作用。观察到1a的主要作用是强效且持续时间长的降压和抗高血压作用，而不会抑制中枢神经系统。
