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

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

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 1...

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Veröffentlicht in:Organic process research & development 2014-01, Vol.18 (1), p.163-167
Hauptverfasser: Reddy, Beeravalli Ramalinga, Reddy, Kikkuru Srirami, Dubey, Manoj Kumar, Kumari, Y. Bharati, Bandichhor, Rakeshwar
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:1083-6160
1520-586X
DOI:10.1021/op400144z