SUPERNUCLEOPHILIC 4-SUBSTITUTED-PYRIDINE CATALYSTS, AND PROCESSES USEFUL FOR PREPARING SAME

• Main Authors: HUCKSTEP L MARK, MURUGAN RAMIAH, BALASUBRAMANIAN MARUDAI, CALVIN JOEL R, CURTIS JOE W, HOPPER CHARLES R, SCRIVEN ERIC F V
• Format: Patent
• Language: English
• Published: 14.02.2008
• Subjects: CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOIDCHEMISTRY; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; PERFORMING OPERATIONS; PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL; THEIR RELEVANT APPARATUS; TRANSPORTING

PROBLEM TO BE SOLVED: To provide processes for producing extrusion-granulated supernucleophilic 4-amino-substituted pyridine catalysts. SOLUTION: The process for producing granular supernucleophilic 4-(secondary or tertiary) aminopyridine catalysts is disclosed which includes the steps of: providing the supernucleophilic catalyst as a molten flowable mass; extruding the molten flowable mass through an orifice into discrete liquid portions each corresponding to a granule to be formed; and cooling these discrete liquid portions. The preferred activation-substitution-deactivation processes for producing 4-aminopyridine compounds are also disclosed which involve the use of acrylic acid or acrylamide or analogs thereof for activation, and substitution steps conducted under mild basic conditions in an excess of the amine reagent for 4-substitution. Such processes provide improved reacted masses which are more readily processed to recover the products in pure, heat-stable forms. Further processes for preparing 4-substituted-pyridines via pyridine betaines are described. COPYRIGHT: (C)2008,JPO&INPIT