Hydrochloric Acid → 5-(Piperidin-4-ylmethoxy)quinazoline-2,4-diamine

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Reaction Steps

4-(2,4-Diamino-quinazolin-5-yloxymethyl)-piperidine-1-carboxylic acid tert-butyl ester (16.4 g; 44.0 mmol) was suspended in 80 mL of dioxane and 4M HCl in dioxane (176 mL, 176 mmol) was added changing the mixture from homogenous to heterogenous. After 5 hrs of stirring at room temperature, solids were filtered off and rinsed once with ether. Solids were triturated with 1 N NaOH for 30 minutes. Solids were collected by filtration and dried to yield 5-(piperidin-4-ylmethoxy)quinazoline-2,4-diamine. (9.05 g; 75% yield).

Provenance & Evidence