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PROBLEM TO BE SOLVED: To provide an intermediate that is useful for the preparation of naftopidil (Naftopidil, (2RS)-1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-(naphthalene-1-yloxy)propan-2-ol), and a method for preparing naftopidil using the same.
SOLUTION: By freeing naftopidil monohydrochloride dihydrate, naftopidil can be obtained in high yield and high purity. In particular, a purity of 99.99% can be achieved without repeating purification operation such as recrystallization multiple times.
SELECTED DRAWING: Figure 1
COPYRIGHT: (C)2021,JPO&INPIT
【課題】ナフトピジル(Naftopidil、(2RS)−1−[4−(2−メトキシフェニル)ピペラジン−1−イル]−3−(ナフタレン−1−イルオキシ)プロパン−2−オ−ル)の調製に有用な中間体およびそれを用いたナフトピジルの調製方法の提供。【解決手段】ナフトピジル一塩酸塩二水和物をフリー化することでナフトピジルを高収率かつ高純度で得ることができる。特に、再結晶等の精製操作を複数回繰り返すことなく、純度99.99%を実現できる。【選択図】図1