An Alternative Indazole Synthesis for Merestinib,Organic Process Research & Development

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An Alternative Indazole Synthesis for Merestinib
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-02-21 00:00:00 , DOI: 10.1021/acs.oprd.8b00016
Yu Lu ₁ , Kevin P. Cole ₁ , Jared W. Fennell ₁ , Todd D. Maloney ₁ , David Mitchell ₁ , Ramesh Subbiah ₂ , Balakumar Ramadas ₂

Affiliation

A new synthesis of a key indazole-containing building block for the MET kinase inhibitor merestinib was designed and demonstrated. Crucial to the successful construction of the challenging indazole is an S_NAr reaction, which forges the heterocyclic ring. Continuous processing was applied to two of the five steps: nitration of a benzaldehyde and high-temperature hydrolysis of an aniline to phenol. Compared to a highly developed historical route, the new route shows clear benefits in terms of product quality and potentially manufacturability and robustness.

中文翻译：

Merestinib的另一种吲唑合成

设计并证明了MET激酶抑制剂merestinib的关键化合物的新合成。成功构建具有挑战性的吲唑的关键是S _N Ar反应，该反应可锻造杂环。对五个步骤中的两个步骤进行了连续处理：苯甲醛的硝化和苯胺的高温水解为苯酚。与高度发展的历史路线相比，新路线在产品质量以及潜在的可制造性和鲁棒性方面显示出明显的优势。

更新日期：2018-02-21

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