Synthesis process of 2, 2, 2-trifluoroacetamidine

• Main Authors: GAO JIAN, YU JURONG
• Format: Patent
• Language: Chinese; English
• Published: 30.08.2022
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

The invention relates to the technical field of pharmaceutical chemical synthesis, in particular to a synthesis process of 2, 2, 2-trifluoroacetamidine, which specifically comprises the following steps: taking trifluoroacetic anhydride as an initial raw material, amidating with p-methoxybenzylamine to obtain 2, 2, 2-trifluoro-N-(4-methoxybenzyl) acetamide, sulfating to obtain 2, 2, 2-trifluoro-N-(4-methoxybenzyl) thioacetamide, reacting with 4-methoxybenzylamine to obtain 2, 2, 2-trifluoro-N-(4-methoxybenzyl) thioacetamide, and reacting with 4-methoxybenzylamine to obtain 2, 2, 2-trifluoro-N-(4-methoxybenzyl) thioacetamide. The preparation method comprises the following steps: carrying out substitution reaction on 2, 2, 2-trifluoro-N-(4-methoxybenzyl) acetamidine and an aminomethanol solution under the action of silver carbonate to obtain 2, 2, 2-trifluoro-N-(4-methoxybenzyl) acetamidine, and carrying out palladium-carbon high-pressure hydrogenation to remove p-methoxybenzyl to obtain 2, 2, 2-trifluoroacetami