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本文报道简化长春胺结构、寻找治疗脑血管疾病有较好疗效的药物。以烯胺Ⅰa,Ⅰb和Ⅰc为起始原料,在C_1位引进羟甲基和羟丙基以及进行酰化等反应,立体选择性地合成了17个结构比长春胺少一个E环的1,2,3,4,6,7,12,12b-八氢-吲哚并[2,3-a]喹嗪衍生物,并分离到3个五环稠合化合物。对于副产物Ⅱ,ⅩⅠⅩ和ⅩⅩ的生成机理作了推测。所合成的化合物进行了小白鼠耐缺氧初筛试验,发现有11个化合物有明显的生物活性,对其它动物的脑血流动力学试验尚在进行中。
This article reports the simplification of vincamine structure and search for drugs that have a good effect in the treatment of cerebrovascular disease. The enamine Ia, Ib and Ic as the starting material, the introduction of hydroxymethyl and hydroxypropyl at the C_1 position and the acylation reaction, the stereoselective synthesis of 17 structures less than vincamine E ring 1, 2,3,4,6,7,12,12b-octahydro-indolo [2,3-a] quinolizine derivatives, and three pentacyclic fused compounds were isolated. The formation mechanism of by-products II, XIX and XX was presumed. The compounds were tested in hypoxia-tolerant mice, and 11 compounds were found to have obvious biological activity. The cerebral hemodynamics test of other animals is still underway.