330457-59-5Relevant articles and documents
Methylphenidate, right pai methyl ester preparation method, intermediate and preparation method
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Paragraph 0304-0312, (2019/04/30)
The invention discloses preparation methods of methylphenidate and dexmethylphenidate, intermediates and preparation methods of the intermediates. The invention provides the preparation method of the methylphenidate, wherein the preparation method is any one of the following methods: a first method comprises the following steps of in a solvent, carrying out an amino protecting group removal reaction of a compound 4 with an amino de-protection reagent, and thus obtaining the methylphenidate 5; a second method comprises the following steps of under the action of an alkali, carrying out an intramolecular nucleophilic substitution reaction of a compound 11 to obtain the methylphenidate 5; and a third method comprises the following steps of in a closed system, in a solvent, under a palladium on carbon or palladium carbon hydroxide catalytic condition, carrying out a reaction of a compound 9 with hydrogen, to obtain the methylphenidate 5. The synthesis method has the advantages of short steps, cheap and easily obtained raw materials, high product yield, good chiral purity, low production cost, and good atomic economy, and is suitable for industrialized production.
Lewis acid-catalyzed ring-opening reactions of semicyclic N,O-acetals possessing an exocyclic nitrogen atom: Mechanistic aspect and application to piperidine alkaloid synthesis
Sugiura,Hagio,Hirabayashi,Kobayashi
, p. 12510 - 12517 (2007/10/03)
Ring-opening reactions of semicyclic N,O-acetals possessing an exocyclic nitrogen atom with silicon-based nucleophiles (silyl enol ethers, ketene silyl acetals, allylic silanes, and trimethylsilyl cyanide) were systematically studied for the first time. I
