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A two-hour synthesis of anti-Parkinson drug Safinamide Methanesulfonate
Synlett ( IF 2 ) Pub Date : 2021-06-22 , DOI: 10.1055/a-1534-0343
Alvaro T. Omori , Vanessa M. Higa

The critical moment of COVID-19 outbreak requires a real time supply of therapeutic agents. Thus, the time economy in the synthesis of biologically active compounds has been increasingly decisive. In this work, we have developed a two-hour synthesis of anti-Parkinson drug safinamide methanesulfonate in 4 steps, with 64% overall yield. Microwave irradiation was used in the first three steps in a one-pot fashion. In fact, this presented protocol can provide Safinamide free base in one hour without chromatographic purification step. Also, green solvents such as methanol and ethyl acetate were applied.

中文翻译:

两小时合成抗帕金森药物 Safinamide Methanesulfonate

COVID-19 爆发的关键时刻需要实时供应治疗剂。因此,生物活性化合物合成中的时间经济性越来越具有决定性。在这项工作中,我们开发了一种 2 小时合成的抗帕金森药物 safinamide 甲磺酸盐,分 4 步,总产率为 64%。在前三个步骤中以一锅方式使用微波辐射。事实上,该方案可以在一小时内提供 Safinamide 游离碱,无需色谱纯化步骤。此外,还使用了绿色溶剂,如甲醇和乙酸乙酯。
更新日期:2021-07-09
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