Optimisation of the synthesis of second generation 1,2,4,5 tetraoxane antimalarials
作者:Paul M. O' Neill、Sunil Sabbani、Gemma L. Nixon、Matthew Schnaderbeck、Natalie L. Roberts、Emma R. Shore、Christopher Riley、Ben Murphy、Paul McGillan、Stephen A. Ward、Jill Davies、Richard K. Amewu
DOI:10.1016/j.tet.2016.08.043
日期:2016.10
An efficient route to the synthesis of potent antimalarial aryloxy 1,2,4,5-tetraoxanes is described that permits parallel synthesis for Structure–Activity Relationship (SAR) investigations. Brief details of the in vitro and in vivo antimalarial evaluation are included which enables identification of antimalarial leads for further development. Also described is an improved approach to the synthesis of
描述了一种有效的合成有效抗疟芳氧基1,2,4,5-四恶烷的有效途径,该方法可用于结构-活性关系(SAR)研究的平行合成。包括体外和体内抗疟疾评估的简短详细信息,使鉴定抗疟疾的线索有待进一步开发。还描述了从市售起始原料仅在四个或五个合成步骤中合成选定的晚期铅化合物的改进方法。