Abstract
Objective: To optimize the synthetic route of rimonabant. Methods: Rimonabant hydrochloride was synthesized from 4-chloropropiophenone as starting material by silylation, acylation with ethyl oxalyl chloride to give α-γ-diketo ester, which was subjected to hydrazone reaction, cyclization, hydrolysis, amidation and salt formation. Results: The structure of the target compound was confirmed by MS, 1HNMR, element analysis, and the overall yield was up to 34.2%. Conclusion: This synthetic route is of mild reacting condition, easy operation and relative high yield and is worthy to be pilot.
| Original language | English |
|---|---|
| Pages (from-to) | 1152-1154 |
| Number of pages | 3 |
| Journal | Chinese Journal of New Drugs |
| Volume | 18 |
| Issue number | 12 |
| State | Published - 30 Jun 2009 |
Keywords
- Antiobesity agent
- Rimonabant
- Synthesis