Continuous Flow Synthesis of Biologically Interesting 2-Aminothiazole Derivatives – mg-Scale Optimisation (Labtrix®) and kg-Scale Production (Kilo-Flow®) of N - (Phenylthiazol-2-yl) acetamide.
With 2-aminothiazoles representing a pharmaceutically important scaffold that possess with wide ranging biological activity such as anti-microbial, ant-bacterial, ant-inflammatory, ant-fungal, anti-HIV and anti-prion, significant research has been undertaken into the construction of combinatorial libraries.
Methods for their preparation include the Hantzsch reaction between a-haloketones and thioureas, a-toszloxzketones or in-situ bromination of acetophenone derivatives. However, despite the large number of biologically active molecules containing the thiazole ring, many reported methods suffer from drawbacks such as harsh reaction conditions, low yields and difficulties in isolating the materials from the solvent system employed.
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