Improved Process for Preparation of (3R,4R)-3-(3,4-Dimethyl-4-piperidinyl)phenol, A Key Intermediate for the Synthesis of Alvimopan

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• 作者：Beeravalli Ramalinga Reddy ; Kikkuru Srirami Reddy ; Manoj Kumar Dubey ; Y. Bharati Kumari ; Rakeshwar Bandichhor
• 刊名：Organic Process Research & Development
• 出版年：2014
• 出版时间：January 17, 2014
• 年：2014
• 卷：18
• 期：1
• 页码：163-167
• 全文大小：279K
• ISSN：1520-586X

文摘

This report discloses an industrially feasible and cost efficient process for the preparation of the compound [(3R, 4R)-3-(3,4-dimethyl-4-piperidinyl)phenol] (1), which is used as the key intermediate for preparation of the opioid drug Alvimopan. The overall yield in this process is increased from 15 to 30%, mainly due to the improvement in yield from 26 to 53% for intermediate 7.