Identification of an Unexpected Impurity in a New Improved Synthesis of Lesinurad,Organic Process Research & Development

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Identification of an Unexpected Impurity in a New Improved Synthesis of Lesinurad
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2018-11-29 00:00:00 , DOI: 10.1021/acs.oprd.8b00316
Aleš Halama ₁ , Jan Stach ₁ , Stanislav Rádl ₁ , Kristýna Benediktová ₁

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An unexpected phenomenon concerning an otherwise common impurity of lesinurad has been observed in the context of synthetic process development. A new industrial process was designed as a chlorine-free process, but the critical chlorinated impurity 10 was surprisingly detected in the isolated product. Because of the structural similarity of the impurity and the product, no efficient separation of 10 by conventional methods (e.g., crystallization) was discovered. The formation of the impurity was explained by a chlorine impurity in a commercial brominating agent. This communication also describes control of the critical impurity.

中文翻译：

莱辛努德的新改进合成中意外杂质的鉴定

在合成方法开发的背景下，已经观察到与莱辛努拉胶原本常见的杂质有关的意想不到的现象。一个新的工业过程被设计为无氯过程，但是在分离出的产品中却发现了关键的氯化杂质10。由于杂质和产物的结构相似，未发现通过常规方法（例如结晶）能有效分离出10种杂质。杂质的形成可以通过商业溴化剂中的氯杂质来解释。该通信还描述了关键杂质的控制。

更新日期：2018-11-29

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