Abstract: The invention relates to processes for preparing acylated amphetamine, methamphetamine and dexamphetamine derivatives by reacting the parent amine with the to be-coupled acid or a salt of the to-be coupled acid which acid is optionally protected, in the presence of an alkylphosphonic acid anhydride as coupling agent and, if the acid was protected then cleaving the protecting group(s), in a one-pot reaction or in two or more separate steps.
Type:
Grant
Filed:
October 9, 2008
Date of Patent:
July 16, 2013
Assignee:
Archimica, Inc.
Inventors:
Andreas Meudt, Richard Wisdom, Jason Helmke, Quofang Qiu, Paul Meek
Abstract: A process for preparing the d-threo isomer of methylphenidate hydrochloride which includes (i) resolving a racemic mixture of racemic threo-methylphenidate hydrochloride with a less than stoichiometric amount of tertiary amine base to obtain a methylphenidate-chiral acid salt, (ii) basifying the methylphenidate-chiral acid salt to obtain methylphenidate free base, and (iii) converting the methylphenidate free base into d-threo-methylphenidate hydrochloride.
Type:
Grant
Filed:
January 5, 2007
Date of Patent:
March 1, 2011
Assignee:
Archimica, Inc.
Inventors:
Alexei Kalinin, Guofang Qiu, Thomas J. Marren, James E. Aldred, Jr., Yu Ji