Synthetic intermediates and improved processes for preparing rock inhibitors
Provided herein are methods of synthesizing netarsudil, and intermediates thereof, in high yield and at large commercial scale. A key intermediate in this synthesis is the preparation of piperidinium (S)-3-((tert-butoxycarbonyl)amino)-2-(4-(((2,4-dimethylbenzoyl)oxy)methyl)phenyl)propanoate, a salt...
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| creator | Thomas Francis Nelson HAXELL Michael Scott MCCLURE Daniel Francis MINKLER |
| description | Provided herein are methods of synthesizing netarsudil, and intermediates thereof, in high yield and at large commercial scale. A key intermediate in this synthesis is the preparation of piperidinium (S)-3-((tert-butoxycarbonyl)amino)-2-(4-(((2,4-dimethylbenzoyl)oxy)methyl)phenyl)propanoate, a salt that has been found to be easily purified by recrystallization. |
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| title | Synthetic intermediates and improved processes for preparing rock inhibitors |
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