HIV非核苷酸逆转录酶抑制剂的合成  

Synthesis of HIV Non-nucleotide Reverse Transcriptase Inhibitors

作　　者：王奕程 Wang Yicheng(Zhejiang Yiwu High School,Jinhua Zhejiang 322000,China)

机构地区：[1]浙江省义乌中学,浙江金华322000

出　　处：《山西化工》2024年第1期37-41,共5页Shanxi Chemical Industry

摘　　要：获得性免疫缺陷综合症作为一种无声、致命的杀手,是当今世界最为严重的传染性疾病之一。逆转录酶是HIV病毒增殖所需的重要蛋白质,目前非核苷酸逆转录酶抑制剂以其较高的特异性而被广泛采用。本文将关注于三种经典的HIV非核苷酸逆转录酶抑制剂Rilpivirine、Etravirine以及Doravirine的化学合成,从最初产率较低、耗时较长的合成出发,通过采用微波辐射、正交实验以及有机金属催化反应达到合成最优化的目的。最优化的过程不仅仅局限于对反应路线的改进,还有在反应路线的基础上小尺度地对反应参数的最优化。Acquired immunodeficiency syndrome,as a silent and deadly killer,is one of the most serious infectious diseases in the world today.Reverse transcriptase is an important protein required for the proliferation of HIV virus,and currently non nucleotide reverse transcriptase inhibitors are widely used due to their high specificity.This article will focus on the chemical synthesis of three classic HIV non nucleotide reverse transcriptase inhibitors,Rilpivirine,Etavirine,and Doravirine.Starting from the initial low yield and time-consuming synthesis,the goal of synthesis optimization is achieved through microwave radiation,orthogonal experiments,and organic metal catalytic reactions.The process of optimization is not limited to improving the reaction route,but also to small-scale optimization of reaction parameters based on the reaction route.

关 键 词：有机合成 有机合成最优化 获得性免疫缺陷综合症 非核苷酸逆转录酶抑制剂 

分 类 号：R914.5[医药卫生—药物化学]