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AssigneeISP Investments Inc.
InventorsArie Gutman, Igor Zaltsman, Anton Shalimov, Maxim Sotrihin, Gennady Nisnevich, Lev Yudovich, Irina Fedotev
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The present invention provides a new and efficient process for the preparation of the dexmethylphenidate hydrochloride with high optical purity, the process comprising: (a) reacting a solution of threo-N-Boc-ritalinic acid with (S)-1-phenylethylamine, separating precipitated solid salt of (R,R)-enriched N-Boc-ritalinic acid with (S)-1-phenylethylamnine from the reaction mixture and recrystallizing, reslurring and/or trituring of said salt; (b) mixing the solid salt of (R,R)-N-Boc-ritalinic acid and (S)-1-phenylethylamine obtained in step (a) with aqueous acid and separating (R,R)-N-Boc-ritalinic acid from the mixture; and (c) reacting the (R,R)-N-Boc-ritalinic acid prepared in step (b) with hydrogen chloride and methanol to give dexmethylphenidate hydrochloride with optical purity of at least 99% ee. The present invention further provides salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine as new intermediate in the preparation of dexmethylphenidate hydrochloride.
A process for the preparation of dexmethylphenidate hydrochloride having high optical purity wherein said threo-N-Broc-ritalinic acid is prepared by a process comprising:
A salt of (R,R)-N-Boc-ritalinic acid with (S)-1-phenylethylamine in a substantially pure solid form of optical purity.
Sodium salt of N-Boc-threo-ritalinic acid in a substantially pure solid form of optical purity.
Dependencies are inferred from the claim text.