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Development and Validation of a Kilogram-Scale Synthesis of Tirapazamine.
ACS Omega ( IF 3.7 ) Pub Date : 2020-07-01 , DOI: 10.1021/acsomega.0c01250
Philippe Lienard 1 , Steven Elenbaas 2
Affiliation  

The process selection and subsequent development of a reliable, scalable synthesis of the anticancer prodrug tirapazamine (SR259075) is described in this paper. Reaction of benzofuroxan with cyanamide in acetonitrile in the presence of 1,8-diazabicyclo[5.4.0]undec-7-ene at 20–25 °C afforded, after an acidic workup, the targeted molecule in good yield at a kilogram scale. Notable critical parameters and safety enhancements are defined and successfully implemented to produce three consecutive validation batches in a reproducible manner.

中文翻译:

公斤级Tirapazamine合成的开发和验证。

本文描述了抗癌前药替拉帕明(SR259075)的可靠,可扩展合成方法的选择和后续开发。在1,8-二氮杂双环[5.4.0]十一碳-7-烯存在下,于20-25°C的条件下,苯并呋喃和乙酰胺在乙腈中反应,经过酸性处理后,得到的目标分子具有良好的千克级收率。定义并成功实施了重要的关键参数和安全性增强功能,从而以可重现的方式生产了三个连续的验证批次。
更新日期:2020-07-14
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