Improved and Practical Synthesis of 6-Methoxy-1,2,3,4- tetrahydroisoquinoline Hydrochloride

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• 作者：H. Marlon Zhong ; Frank J. Villani ; Ramzy Marzouq
• 刊名：Organic Process Research & Development
• 出版年：2007
• 出版时间：May 2007
• 年：2007
• 卷：11
• 期：3
• 页码：463 - 465
• 全文大小：32K
• 年卷期：v.11,no.3(May 2007)
• ISSN：1520-586X

文摘

6-Methoxy-1,2,3,4-tetrahydroisoquinoline (1) or its hydrochloride salt (4) is an expensive chemical with limited commercialavailability. We report an improved and practical synthesis of4 from inexpensive 2-(3-methoxyphenyl)ethylamine (2) using aPictet-Spengler condensation via a novel aminal intermediate.The synthesis significantly lowers the cost and provides easyaccess to 6-methoxy-1,2,3,4-tetrahydroisoquinoline or its HClsalt on a large scale.