These common heterocyclic compound, 29671-92-9, name is Carbamimidic chloride hydrochloride, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. Safety of Carbamimidic chloride hydrochloride
To a solution of the ethyl [2-(4-{3-[(tert-butoxycarbonyl)amino]propoxy}-phenyl)cyclopropyl]acetate (Step 6, Example 1, 3.52 g, 0.01 mol) in dry dichloromethane (20 mL) was added 4N HCl in dioxane (12.5 mL, 0.05 mol). The solution was stirred at room temperature for 2 hours and solvent evaporated to give white solid as HCl salt. To a solution of carbamidic chloride hydrochloride (2.03 g, 0.0176 mol) in acetonitrile (30 mL) and triethylamine (11 mL) was added crude amine (2.75 g, 0.0088 mol) in acetonitrile (20 mL). The reaction mixture was refluxed overnight and solvent concentrated to give solid residue used without further purification. The mass spectrum was consistent with the proposed structure. M+=320.
The synthetic route of Carbamimidic chloride hydrochloride has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Nagarajan, Srinivasan R.; Khanna, Ish Kumar; Clare, Michael; Gasiecki, Alan; Rogers, Thomas; Chen, Barbara; Russell, Mark; Lu, Hwang-Fun; Yi, Yu; Huff, Renee M.; Desai, Bipinchandra N.; Devadas, Balekudru; Parikh, Mihir D.; Penning, Thomas; US2004/92538; (2004); A1;,
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