A PROCESS FOR PREPARING 2-HYDROXY-3- [5- (MORPHOLIN-4-YLMETHYL)PYRIDIN-2-YL] LH-INDOLE-5-CARBONITRILE AS A FREE BASE OR SALTS THEREOF

摘要

The present invention relates to a new process for the manufacture of the compound 2-hydroxy-3-[5-(mofholin-4-ylmethyl)pyridin-2-yl]lH'-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the 2-hydroxy-3-[5- (morpholm-4-ylmethyl)pyridin-2-yl]lH-indole-5-carbonitrile citrate, to the use of said compounds for the manufacturing of a medicament for the treatment of cognitive disorders, Alzheimer disease, dementias, chronic and acute neurodegenerative diseases, bipolar disorders, schizophrenia, diabetes, hair loss etc. and to new intermediates as well as a robust condition for catalytic cyanation for the preparation of 2-hydroxy-3-[5- (mofholin-4-yhnethyl)pyridin-2-yl]lH-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, and to a new intermediate prepared in said process suitable for large scale manufacturing of said compounds.The invention also relates to a new use in cyanation reaction of palladium catalysts.