IMPROVED METHOD FOR MAKING NEVIRAPINE

IMPROVED METHOD FOR MAKING NEVIRAPINE

A PROCESS FOR MAKING NEVIRAPINE, COMPRISING THE FOLLOWING STEPS: (A) REACTING A 2-HALO-3-PYRIDINECARBONITRILE OF THE FORMULA WHEREIN X IS A FLUORINE, CHLORINE, BROMINE OR IODINE ATOM, PREFERABLY CHLORINE OR BROMINE, WITH CYCLOPROPYLAMINE, TO YIELD 2-(CYCLOPROPYLAMINO)- 3-PYRIDINECARBONITRILE; (B) HY...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: ROBERT FREDERICK BOSWELL, YOUNG SEK LO, FRANKLIN GUPTON
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:A PROCESS FOR MAKING NEVIRAPINE, COMPRISING THE FOLLOWING STEPS: (A) REACTING A 2-HALO-3-PYRIDINECARBONITRILE OF THE FORMULA WHEREIN X IS A FLUORINE, CHLORINE, BROMINE OR IODINE ATOM, PREFERABLY CHLORINE OR BROMINE, WITH CYCLOPROPYLAMINE, TO YIELD 2-(CYCLOPROPYLAMINO)- 3-PYRIDINECARBONITRILE; (B) HYDROLYZING THE 2-(CYCLOPROPYLAMINO)-3-PYRIDINECARBONITRILE TO YIELD 2(CYCLOPROPYLAMINO)-3-PYRIDINE CARBOXYLIC ACID; (C) ISOLATING THE 2-(CYCLOPROPYLAMINO)-3-PYRIDINE CARBOXYLIC ACID FROM THE REACTION MEDIUM; (E) TREATING THE 2-(CYCLOPROPYLAMINO)-3-PYRIDINE CARBOXYLIC ACID WITH A CHLORINATING AGENT, TO YIELD 2-( CYCLOPROPYLAMINO)-3-PYLIDINECARBONYL CHLORIDE; (F) REACTING THE 2-(CYCLOPROPYLAMINO)-3-PYRIDINE CARBONYL CHLORIDE WITH A 2-HALO-4-METHYL-3- PYRIDINAMINE OF THE FORMULA WHEREIN X IS A FLUORINE, CHLORINE, BROMINE OR IODINE ATOM, PREFERABLY CHLORINE OR BROMINE, TO PRODUCE AN N-(2-HALO-4-METHYL-3-PYRIDINYL)-2-( CYCLOPROPYLAMINO )-3PYRIDINECARBOXAMIDE; AND (G) CYCLIZING THE N-(2-HALO-4-METHYL-3-PYRIDINYL)-2-(CYCLOPROPYLAMINO)-3PYRIDINECARBOXAMIDE BY TREATMENT WITH A STRONG BASE, TO YIELD NEVIRAPINE.