Abstract: The process comprises reacting a compound of formula (II), where R is a hydroxyl protecting group, and the asterisk indicates an asymmetric carbon atom, with diisopropylamine in the presence of a reducing agent; optionally converting the resulting intermediate into a salt and, if so desired, isolating it; removing the hydroxyl protecting group; and if so desired, separating the desired (R) or (S) enantiomer, or the mixture of enantiomers and/or converting the obtained compound into a pharmaceutically acceptable salt thereof. Tolterodine is a muscarinic receptor antagonist useful in treating urinary incontinence and other symptoms of urinary bladder hyperactivity.
Type:
Grant
Filed:
December 21, 2004
Date of Patent:
January 6, 2009
Assignee:
Ragactives, S.L. Parque Tecnologico de Boecillo
Inventors:
Gustavo Pascual Coca, Pablo Martin Pascual, Jorge Martin Juarez