Synthesis of a stable Triformylmethane (cas 18655-47-5) synthon and its scalable application to 7-acylamino-3-formylquinoline syntheses

Add time:09/09/2019    Source:sciencedirect.com

Novel 2-iminiomethylvinamidinium trihalides were isolated as stable crystals and found to be useful Triformylmethane (cas 18655-47-5) synthons with non-deliquescent nature in air. They were easier to manufacture, handle, and store than the known 2-iminiomethylvinamidinium dichloride. By virtue of in situ aminal protection, a combination of the vinamidinium salt with a secondary amine achieved an efficient and scalable synthesis of 7-acylamino-3-formylquinoline, a versatile synthetic intermediate for potent anti-obesity drugs 7-acylamino-3-aminomethyl-8-methylquinolines.

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