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Continuous flow aminolysis under high temperature and pressure
Journal of Flow Chemistry ( IF 2.0 ) Pub Date : 2020-02-05 , DOI: 10.1007/s41981-019-00049-6
Bryan Li , Scott Bader , Steve M. Guinness , Sally Gut Ruggeri , Cheryl M. Hayward , Steve Hoagland , John Lucas , Ruizhi Li , David Limburg , J. Christopher McWilliams , Jeffrey Raggon , John Van Alsten

Under continuous processing conditions, C-N bond formation via SN2 and SNAr substitutions by amines can be an effective preparative method, especially when volatile amines are used under high pressure and temperature. We have demonstrated SN2 substitution of a 2° mesylate with ammonia and opening of an epoxide with benzylamine, and SNAr substitution of a heteroaryl chloride with aqueous ammonia on multi-kg scales. The homogeneous continuous processes offered better process control, higher efficiency, and comparable or superior reaction profiles and yields to batch conditions.

Continuous flow aminolysis under high temperature and pressure



中文翻译:

高温高压连续流氨解

在连续加工条件下,通过SN 2形成CN键和用胺取代SNAr可能是一种有效的制备方法,尤其是在高压和高温下使用挥发性胺时。我们已经证明了用氨水将2°甲磺酸盐进行SN 2取代,并用苄胺打开了环氧化物,以及用氨水将杂芳基氯的SNAr取代了几千克规模。均匀的连续过程可提供更好的过程控制,更高的效率,以及可与批处理条件相比或更高的反应曲线和产率。

高温高压连续流氨解

更新日期:2020-02-05
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