An efficient synthesis of Ceritinib (LDK378) using a Sandmeyer reaction

Liu Haidong; Li Yuan; Wang Dongdong; Qin Yu; Ji Min

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An efficient synthesis of Ceritinib (LDK378) using a Sandmeyer reaction

机译：使用Sandmeyer反应有效合成Ceritinib（LDK378）

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A convenient route for the synthesis of Novartis's second-generation anaplastic lymphoma kinase inhibitor Ceritinib (LDK378) involving starting materials that are commercially available has been achieved. The procedure employed mild reaction conditions and avoided the use of expensive reagents compared to the original synthetic route reported by Novartis. More importantly, gram scale synthesis was accomplished and this protocol could be valid in drug discovery synthesis.

机译：已经实现了一种合成诺华第二代间变性淋巴瘤激酶抑制剂Ceritinib（LDK378）的简便途径，其中涉及可商购的原料。与诺华报道的原始合成路线相比，该程序采用了温和的反应条件，避免了使用昂贵的试剂。更重要的是，完成了克级合成，该方案在药物发现合成中可能是有效的。

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《Journal of chemical research: reviews and research papers from all branches of chemistry》 |2015年第8期|共3页
作者
Liu Haidong; Li Yuan; Wang Dongdong; Qin Yu; Ji Min;
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正文语种 eng
中图分类化学;
关键词
ceritinib; LDK378; Sandmeyer reaction; diazonium salts; 2; 4-dichloro-5-nitropyrimidine;

机译：ceritinib;LDK378;Sandmeyer反应;重氮盐;2;4-二氯-5-硝基嘧啶;

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1. An efficient synthesis of Ceritinib (LDK378) using a Sandmeyer reaction [J] . Liu Haidong, Li Yuan, Wang Dongdong, Journal of chemical research: reviews and research papers from all branches of chemistry . 2015,第8期

机译：使用Sandmeyer反应有效合成Ceritinib（LDK378）
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An efficient synthesis of Ceritinib (LDK378) using a Sandmeyer reaction

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