- One Synthetic Approach of Eflornithine hydrochloride hydrate
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hydrochloride hydrate (CAS NO.: ), with other name of 2-Difluoromethyl-DL-ornithine monohydrochloride monohydrate, could be produced through the following synthetic routes.
The reaction routes are as below:
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The optical resolution of 2,5-diamino-2-(difluoromethyl)pentanoic acid is performed as follows: The cyclization of its corresponding (I) by means of sodium methoxide in methanol gives the racemic piperidone (II), which is submitted to optical resolution with (-)-binaphthylphosphoric acid yielding after crystallization and acidification with HCl the (+) and (-) piperidones (III) and (IV). Finally, both compounds are treated with refluxing 6N HCl to afford the target enantiomers.
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