摘要 |
PURPOSE:To effect the reaction between a carboxylic acid and cyanamide in an aqueous solution of prescribed pH value to produce a guanidino compound which is used as a synthetic intermediate of medicines. CONSTITUTION:A compound of formula I (A is formula II, III; n is 1, 2) is allowed to react with cyanamide in an aqueous solution of over 9 pH. A base such as ammonia is added to the reaction system in order to keep the pH over 9. An equimolar or more amount, preferably 1.5-3 times molar amount of cyanamide is used based on the compound of formula I and the reaction is carried out at a temperature higher than 10 deg.C to give the subject compound of formula IV. An example of compounds of formula I is trans-4- aminomethylcyclohexanecarboxylic acid.
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