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Highly Productive Continuous Flow Synthesis of Di- and Tripeptides in Water
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2017-09-14 00:00:00 , DOI: 10.1021/acs.oprd.7b00214
Katherine E. Jolley 1 , William Nye 1 , Carlos González Niño 1 , Nikil Kapur 1 , Alain Rabion 2 , Kai Rossen 3 , A. John Blacker 1
Affiliation  

The reaction of amino acid derived N-carboxyanhydrides (NCAs) with unprotected amino acids under carefully controlled aqueous continuous flow conditions realized the formation of a range of di- and tripeptide products in 60–85% conversion at productivities of up to 535 g·L–1h–1. This required a fundamental understanding of the physicochemical aspects of the reaction resulting in the design of a custom-made continuous stirred tank reactor (CSTR) with continuous solids addition, high shear mixing, automated pH control to avoid the use of buffer, and efficient heat removal to control the reaction at 1 ± 1 °C.

中文翻译:

水中二肽和三肽的高产连续流合成

氨基酸衍生的N-羧基酐(NCA)与未保护的氨基酸在精心控制的水性连续流动条件下的反应实现了一系列二肽和三肽产物的形成,产率高达535 g·L,转化率为60-85%–1小时–1。这需要对反应的物理化学方面有基本的了解,因此需要设计定制的连续搅拌釜反应器(CSTR),其中需要连续添加固体,高剪切混合,自动pH控制以避免使用缓冲液和有效加热除去以将反应控制在1±1°C。
更新日期:2017-09-15
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