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1. JP2021104982 - NAFTOPIDIL MONOHYDROCHLORIDE DIHYDRATE AND USE THEREOF FOR PREPARATION OF NAFTOPIDIL

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Office
Japan
Application Number 2019237681
Application Date 27.12.2019
Publication Number 2021104982
Publication Date 26.07.2021
Publication Kind A
IPC
C07D 295/096
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
04with substituted hydrocarbon radicals attached to ring nitrogen atoms
08substituted by singly bound oxygen or sulfur atoms
096with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
Applicants IWAKI SEIYAKU CO LTD
岩城製薬株式会社
Inventors YOSHIDA YUSUKE
吉田　裕介
FUKUSHIMA KOICHI
福島　孝一
Agents 紺野　昭男
井波　実
伊藤　武泰
田村　慶政
Title
(EN) NAFTOPIDIL MONOHYDROCHLORIDE DIHYDRATE AND USE THEREOF FOR PREPARATION OF NAFTOPIDIL
(JA) ナフトピジル一塩酸塩二水和物およびナフトピジル調製のためのその使用
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Abstract
(EN)

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


(JA)

【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
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