CAJ | 학술논문

泰诺福韦是制备抗病毒药物泰诺福韦酯富马酸盐的关键中间体，以腺嘌呤和（ R）－1，2－亚丙基碳酸酯为原料，经开环缩合、取代和水解3步反应制得泰诺福韦。反应过程用高效液相色谱仪（ HPLC ）进行监测，探讨了反应的最佳工艺：①开环缩合的最佳反应温度为145℃，最佳反应时间为5．5 h；②以叔丁醇镁为碱，取代反应的最佳反应时间为10 h；③采用廉价的三甲基氯硅烷和溴化钠进行水解，最佳反应时间为24 h。在最优化的条件下总收率达到49．6％。
태낙복위시제비항병독약물태낙복위지부마산염적관건중간체，이선표령화（ R）－1，2－아병기탄산지위원료，경개배축합、취대화수해3보반응제득태낙복위。반응과정용고효액상색보의（ HPLC ）진행감측，탐토료반응적최가공예：①개배축합적최가반응온도위145℃，최가반응시간위5．5 h；②이숙정순미위감，취대반응적최가반응시간위10 h；③채용렴개적삼갑기록규완화추화납진행수해，최가반응시간위24 h。재최우화적조건하총수솔체도49．6％。
Tenofovir is the key intermediate for the antiviral drug tenofovir disoproxil fumarate .Tenofovir is synthesized by adenine and propyl carbonate through ring -opening condensation , substitution reaction and hydrolysis reaction .The process of reaction is monitored by using High Performance Liquid Chromatography ( HPLC) .The optimal reaction conditions are discussed:①The best synthesis condition of ring -opening condensation is at 145 ℃ for 5.5 h.②The best reaction time of substitution reaction is 10 h with magnesium tert-butoxide as alkali .③The best reaction time of hydrolysis reaction is 24 h using cheap trimethylchlorosi-lane and sodium bromide.The overall yield of 49.6 % is obtained under optimal conditions.