In the case that a selectively monoacylated phenylenediamine derivative of the following formula:
wherein R1, R2, R3 and R10 have the meanings given in the description which is useful as any of medicines, agricultural chemicals, animal drugs and the intermediates of chemicals is prepared by reacting a benzoic acid derivative with a phenylenediamine derivative, the benzoic acid derivative is converted into a benzoyl imidazole derivative and this benzoyl imidazole derivative is then reacted with the phenylenediamine derivative, whereby the improvement of a preparation efficiency and the high selectivity of the monoacylation can be achieved, the steps of protection and deprotection being omitted.
如果下式为选择性单乙酰化
苯二胺衍
生物:
其中 R1、R2、R3 和 R10 具有说明中给出的含义,该衍
生物可用作药物、农药、动物用药和
化学中间体中的任何一种,是通过
苯甲酸衍
生物与
苯二胺衍
生物反应制备的、将
苯甲酸衍
生物转化为苯甲酰基
咪唑衍
生物,然后将苯甲酰基
咪唑衍
生物与
苯二胺衍
生物反应,从而提高制备效率和单酰化的高选择性,省略保护和脱保护步骤。