Starting from sodium azide, methyl-bromoacetate, and 3-methylbut-1-yne, a safe and efficient three-step continuous process was developed to obtain 2-(4-isopropyl-1H-1,2,3-triazol-1-yl)acetic acid. Isolation of hazardous intermediates was avoided, and by using FT-IR in-line monitoring of the azides involved, risks associated with these components were minimized. Furthermore, the use of FT-IR as a tool for optimization in real time facilitated the understanding of the kinetics of the reaction steps and resulted in a rapid optimization of parameters. The continuous method was used for multihundred grams manufacturing of the triazole which was used as a key building block in one of our drug development projects.

中文翻译：

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开发2-（4-异丙基-1 H -1,2,3-三唑-1-基）乙酸的安全连续生产路线

从叠氮化钠，溴乙酸甲酯和3-甲基丁-1-炔开始，开发了一种安全有效的三步连续方法，以获得2-（4-异丙基-1 H -1,2,3-三唑-1 -基）乙酸。避免了危险中间体的分离，并且通过使用FT-IR在线监测所涉及的叠氮化物，将与这些组分相关的风险降至最低。此外，使用FT-IR作为实时优化工具有助于对反应步骤动力学的理解，并导致参数的快速优化。连续法用于三唑的数百克生产，三唑被用作我们药物开发项目之一的关键组成部分。