高效大量合成AF-5的中间体:(4aR,7R)-1-丁基-4a-甲基-7-(1-甲基-1-羟乙基)-2(1H)-八氢萘酮(英文)

Efficient and Large-Scale Synthesis of an Intermediate of AF-5:(4aR,7R)-1-Butyl-4a-methyl-7-(1-methyl-1-hydroxyethyl)-2(1H)-octalone

化合物(4 aR,7R)-1-丁基-4 a-甲基-7-(1-甲基-1-羟乙基)-2(1H)-八氢萘酮是合成AF-5的重要中间体,传统方法是在强碱叔丁醇钾的作用下对化合物(4 aR,7R)-4 a-甲基-7-(1-甲基-1-羟乙基)-2(1H)-八氢萘酮进行烷基化反应而得到的.为了使操作更方便、安全,适合大量制备,并提高收率,作者探索了多种碱性条件,并选择氢氧化钾的叔丁醇溶液代替叔丁醇钾,最终使该步烷基化反应可以工业化.

For the purpose of safety, the alkylation of （ 4aR, 7R ） -1-butyl-4a-methyl-7- （ 1-methyl-1- hydroxyethyl）-2（1H）-octalone can be fulfilled by using the mild base KOH./t-BuOH replacing the strong base of t-BuOK / t-BuOH. This method is applicable to a large scale for safe synthesis, and optimized reaction conditions have been investigated.