Ceralasertib合成路线图解

Graphical synthetic routes of ceralasertib

Ceralasertib(AZD-6738,1),中文化学名称为4-{4-[(3R)-3-甲基吗啉-4-基]-6-[1-(R)-S-甲基亚磺酰亚氨基环丙基]嘧啶-2-基}-1H-吡咯并[2,3-b]吡啶,英文化学名称为4-(4-(3R)-3-methylmorpholin-4-yl)-6-(1-(R)-S-methylsulfonimidoyl)(cyclopropyl pyrimidin-2-yl)-1H-pyrrolo[2,3-b]pyridine,分子式为C_(20)H_(24)N_(6)O_(2)S,分子量为412.512,CAS登记号为1352226-88-0。

Ceralasertib is a highly selective ataxia telangiectasia mutated and rad3 related kinase(ATR) inhibitor,developed by Astra Zeneca,which has an IC;value of 7 nmol·L;for ATR,and has a selectivity of more than 60 times for the mammalian target of Rapamycin(mTOR) and excellent solubility and good cell(HT29) potency and pharmacokinetic properties. This paper reviews the synthetic methods of ceralasertib,which provides a reference for the large-scale preparation of ceralasertib.