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参考文献:一种克里唑替尼中间体制备方法
标题:一种克里唑替尼中间体制备方法
摘要:本发明为抗肿瘤分子靶向药物克里唑替尼的合成方法,属于制药领域.涉及一种克里唑替尼中间体的合成方法,包括两种还原工艺,一种溴代反应工艺,反应步骤如下:还原工艺一:化合物(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑硝基吡啶与连二硫酸钠,在机械化学条件下发生还原反应,反应生成(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑氨基吡啶;还原工艺二:化合物(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑硝基吡啶溶于有机溶剂中,催化加氢,还原反应生成(R)‑3‑[1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑2‑氨基吡啶;溴代反应工艺:将上述化合物与过硫酸氢钾和溴化盐反应,得到克里唑替尼中间体.该工艺成本低,原材料易购买,操作简便安全,收率高,适用于大规模生产.

专利信息

专利号:CN-118324790-A
优先权日:2024-04-16
标 题 :A method for photocatalytic synthesis of crizotinib intermediates

专利号:US-8785632-B2
优先权日:2004-08-26
标 题:Enantiomerically pure aminoheteroaryl compounds as protein kinase inhibitors
发明人：CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE
权利人:CUI JINGRONG JEAN; FUNK LEE ANDREW; JIA LEI; KUNG PEI-PEI; MENG JERRY JIALUN; NAMBU MITCHELL DAVID; PAIRISH MASON ALAN; SHEN HONG; TRAN-DUBE MICHELLE; AGOURON PHARMA; PFIZER
摘要:Enantiomerically pure compound of formula 1 n nare provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.