叔丁喘宁的合成工艺改进

Improvement of Terbutaline sulphate synthesis

针对目前国内叔丁喘宁合成收率较低的情况, 提出一条新的合成路线. 以3, 5 二羟基苯甲酸为起始原料, 经过酯化、苄基保护、水解、酰化、溴代、胺化、还原和脱苄等八步反应合成叔丁喘宁, 总收率达33 15%. 所有原料全部国产化, 各步反应简单, 最后五步反应总收率达48 04%, 大大降低了工艺成本, 适合工业生产.

Synthesis of Terbutaline sulfate from 3′,5′-dihydroxybenzoic acid was performed in an eight step process. The yield of Terbutaline sulfate was 33.15%, which was 12.5% higher than that reported before. Reaction conditions were mild and the process was simple. A low cost industrial method for the synthesis of Terbutaline sulfate is reported.