摘要
以2-氟-5-溴甲基苯甲酸甲酯为原料,与儿茶酚硼烷进行硼酸化反应制得3-甲氧羰基-4-氟苄基硼酸,与4-氯-1(2H)-酞嗪酮发生Suzuki偶联得2-氟-5-[(4-氧代-3,4-二氢酞嗪-1-基)甲基]苯甲酸甲酯,然后与1-环丙甲酰基哌嗪经缩合反应制得抗肿瘤药奥拉帕尼,总收率为84%。
Olaparib was synthesized from methyl 5-bromomethyl-2-fluorobenzoate by reaction with catecholborane to give 4-fluoro-3-methoxycarbonylbenzylboronic acid, which was subjected to Suzuki coupling reaction with 4-chloro-2H-phthalazin-l-one, followed by condensation with 1-（cyclopropylcarbonyl）piperazine with an overall yield of 84 %.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2016年第8期996-998,共3页
Chinese Journal of Pharmaceuticals
关键词
奥拉帕尼
卵巢癌
合成工艺
olaparib
ovarian cancer
synthetic process
