摘要
4-(3-哌啶基)苯胺是PARP抑制剂尼拉帕尼的重要合成中间体。本文以对硝基苯乙酸为原料,通过酯化、Michael加成、还原,最终成盐合成了4-(3-哌啶基)苯胺及其酒石酸盐,该方法原料易得,成本低廉,操作简单。
4-(Piperidin-3-yl)anitine isan important synthetic intermediate for Niraparib, a PARP inhibitor. A novel synthesis for it has been developed with p-nitrophenylacetic acid as starting material, which includesesterification, Michael addition, reduction and salt formation.The method has convenient and economic advantages.
出处
《广东化工》
CAS
2017年第11期4-5,共2页
Guangdong Chemical Industry