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Fully Continuous Flow Synthesis of 5-(Aminomethyl)-2-methylpyrimidin-4-amine: A Key Intermediate of Vitamin B<sub>1</sub>

Meifen Jiang, Minjie Liu, Hua‐Shan Huang, Fen‐Er Chen

2021Organic Process Research & Development17 citationsDOI

Abstract

Herein, we demonstrate an expeditiously fully continuous flow synthesis of 5-(aminomethyl)-2-methylpyrimidin-4-amine, a key intermediate for vitamin B1. The process is accomplished via three chemical transformations in six sequential continuous flow devices from an economical starting material, 2-cyanoacetamide. First, single step continuous flow synthesis is demonstrated in a certain type of flow reactor for each reaction step, with a yield of 94, 90, and 99%, respectively. Then, fully continuous flow synthesis of 5-(aminomethyl)-2-methylpyrimidin-4-amine is demonstrated in 84% total yield with a total residence time of 74 min and 0.92 g/h throughput.

Topics & Concepts

Yield (engineering)Continuous flowAmine gas treatingChemistryContinuous reactorFlow chemistryCombinatorial chemistryOrganic chemistryMaterials scienceCatalysisMechanicsMetallurgyPhysicsInnovative Microfluidic and Catalytic Techniques InnovationNanomaterials for catalytic reactionsMicrofluidic and Capillary Electrophoresis Applications