1239--9--3-[2--1--1-]-4--4- PROCESS FOR THE PREPARATION OF 1239-TETRAHYDRO-9-METHYL-3-[2-METHYL-1H-IMIDAZOL-1-YLMETHYL]-4H-CARBAZOL-4-ONE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

1239--9--3-[2--1--1-]-4--4- PROCESS FOR THE PREPARATION OF 1239-TETRAHYDRO-9-METHYL-3-[2-METHYL-1H-IMIDAZOL-1-YLMETHYL]-4H-CARBAZOL-4-ONE OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

PURPOSE: Provided is a novel manufacturing method of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on or its pharmaceutically acceptable salt in higher yield and purity than conventional methods. CONSTITUTION: The manufacturing method is characterized by reacting 1,2,3,9-...

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Bibliographische Detailangaben
Hauptverfasser: LEE, GWANG OK, JUNG, GEUM SIN, KIM, GI EUN, LEE, HOE CHEOL, KIM, MAENG SEOP, LEE, GWAN SUN, KIM, HUI SEOK, HAM, YEONG JIN, KIM, CHEOL GYEONG, KIM, HAN GYEONG
Format: Patent
Sprache:eng ; kor
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Zusammenfassung:PURPOSE: Provided is a novel manufacturing method of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on or its pharmaceutically acceptable salt in higher yield and purity than conventional methods. CONSTITUTION: The manufacturing method is characterized by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-on of the formula(2) with 2-methylimidazole derivative of the formula(3) in a mixed solvent of organic solvent and water at room temperature to 150 deg.C fro 2-12 hours to manufacture 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl))-4H-carbazol-4-on of the formula(1) or its pharmaceutically acceptable salt. 본 발명은 할로실란 화합물 존재하에서 하기 화학식 2의 1,2,3,9-테트라히드로-9-메틸-4H-카바졸-4-온을 화학식 3의 2-메틸이미다졸 유도체와 유기용매 또는 유기용매와 물의 혼합용매 중에서 반응시키는 것을 특징으로 하는, 화학식 1의 1,2,3,9-테트라히드로-9-메틸-3-[(2-메틸-1H-이미다졸-1-일)메틸]-4H-카바졸-4-온 또는 그의 약제학적으로 허용가능한 염의 제조 방법에 관한 것으로, 본 발명의 방법에 따르면 보다 간단한 공정으로 목적 화합물을 고수율, 고순도로 제조할 수 있다. 상기 식에서, R은 N,N-디메틸아미노, N,N-디에틸아미노, N,N-디프로필아미노, 몰포린-4-일, 피페리딘-1-일 또는 피롤리딘-1-일이다.