NOVEL PROCESSES FOR PREPARING DIAMINOPYRIMIDINE DERIVATIVE OR ACID ADDITION SALT THEREOF

To provide novel processes for preparing diaminopyrimidine derivatives or acid addition salts thereof, and to provide stable crystalline forms of hydrochlorides of diaminopyrimidine derivatives and processes for preparing the same.SOLUTION: An industrial production method for a diaminopyrimidine derivative, represented by the following formula, involves reacting a guanidine derivative with methyl 3-oxohexanoate to yield a pyrimidine derivative. This is followed by sulfonylation of the hydroxyl groups and subsequent reaction with acetamidopyrrolidine, resulting in the intended product. There are also provided stable crystalline forms A of hydrochlorides.SELECTED DRAWING: Figure 1 【課題】ジアミノピリミジン誘導体またはその酸付加塩を製造する方法、ならびにジアミノピリミジン誘導体の塩酸塩の安定な結晶形およびその製造方法を提供する。【解決手段】下記式で表されるジアミノピリミジン誘導体の工業的製造法は、グアニジン誘導体と３－オキソヘキサン酸メチルとを反応させピリミジン誘導体とした後、水酸基をスルホニル化し、アセトアミドピロリジンと反応させて目的物を得る方法である。また、安定な形態である塩酸塩の結晶形Ａを提供する。JPEG2024056922000025.jpg58166【選択図】図１