摘要
根据起始原料不同对尼拉帕尼的10种合成方法进行了综述。其中以4-溴苯基乙酸为和1-溴-3-氯丙烷为起始原料,经缩合、环化、还原、氨化、保护,然后再与吲唑偶合反应后通过手性拆分的方法产率最高,适合工业化大生产。
Ten different synthetic methods of niraparib were reviewed.The analysis shows that the method using 4-bromophenylacetic acid and 1-bromo-3-chloropropane as starting materials,after condensation,cyclization,reduction,ammonification and protection,and then coupling with indazole has the advantages of high chiral resolution yield,which is suitable for industrial production.
作者
陈慧杰
王秀军
Chen Huijie;Wang Xiujun(School of Pharmacy,Jiangsu Ocean University,Lianyungang 222005,Jiangsu,China)
出处
《精细石油化工》
CAS
2022年第6期79-81,共3页
Speciality Petrochemicals
基金
江苏海洋大学校级课题(KQ20014)。
关键词
尼拉帕尼
卵巢癌
合成
niraparib
ovarian cancer
synthesis
