Sagandira, Cloudius R.; Watts, Paul published the artcile< Rapid Multigram-Scale End-to-End Continuous-Flow Synthesis of Sulfonylurea Antidiabetes Drugs: Gliclazide, Chlorpropamide, and Tolbutamide>, Related Products of 94-20-2, the main research area is chlorpropamide gliclazide tolbutamide continuous flow preparation antidiabetic agent.
A multigram-scale robust, efficient, and safe end-to-end continuous-flow process for the diabetes sulfonylurea drugs gliclazide, chlorpropamide, and tolbutamide is reported. The drugs were prepared by the treatment of an amine with a haloformate affording carbamate, which was subsequently treated with a sulfonamide to afford sulfonylurea. Gliclazide was obtained in 87% yield within 2.5 min total residence time with 26 g/h throughput; 0.2 kg of the drug was produced in 8 h of running the system continuously. Chlorpropamide and tolbutamide were both obtained in 94% yield within 1 min residence time with 184-188 g/h throughput; 1.4-1.5 kg of the drugs was produced in 8 h of running the system continuously. N-Substituted carbamates were used as safe alternatives to the hazardous isocyanates in constructing the sulfonyl urea moiety.
Synthesis published new progress about Antidiabetic agents. 94-20-2 belongs to class amides-buliding-blocks, and the molecular formula is C10H13ClN2O3S, Related Products of 94-20-2.
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