As for this invention, being production manner of the salt which it can allow the paliperidone or as that medicine, the ideal solvent and in the base, under existing of the catalytic converter and the inhibiter, the chemical compound formula (ii) the chemical compound or that salt formula (iii) being to make condense, the said inhibiter, as for the front stirrup where react with the chemical compound formula (ii) and the chemical compound formula (iii) when the reaction with the chemical compound formula (ii) and the chemical compound formula (iii) starts, is something which is added to the said reaction system here, and, optionally the paliperidone transforming in that salt (in formula, XIt is the ideal desorption basis) it includes, aforementioned production manner is offered. This invention, the paliperidone which substantially is produced the pure paliperidone or that salt, by the said manner or that salt, the paliperidone or offers the use of that salt.< Conversion 1 >< Choice figure >It is not本発明は、パリペリドン又はその医薬として許容し得る塩の製造方法であって、好適な溶媒及び塩基中、触媒及び阻害剤の存在下、式(II)の化合物を式(III)の化合物又はその塩と縮合させることであって、ここで該阻害剤が、式(II)の化合物と式(III)の化合物とが反応する前又は式(II)の化合物と式(III)の化合物との反応が開始する時に該反応系に添加されるものであり、並びに、任意にパリペリドンをその塩に転化すること(式中、Xは好適な脱離基である)を含む、前記製造方法を提供する。本発明は、実質的に純粋なパリペリドン又はその塩、該方法により製造されたパリペリドン又はその塩、パリペリドン又はその塩の使用を提供する。【化1】【選択図】なし
