METHOD FOR PREPARING (3-CHLORO-4-FLUOROPHENYL)-(4-FLUORO-4-{[(5METHYL-PYRIMIDIN-2-YLMETHYL)-AMINO]-METHYL}-PIPERIDIN-1-YL)-METHANONE AND NOVEL INTERMEDIATE PYRIMIDINE DERIVATIVES

METHOD FOR PREPARING (3-CHLORO-4-FLUOROPHENYL)-(4-FLUORO-4-{[(5METHYL-PYRIMIDIN-2-YLMETHYL)-AMINO]-METHYL}-PIPERIDIN-1-YL)-METHANONE AND NOVEL INTERMEDIATE PYRIMIDINE DERIVATIVES

Preparation of (3-chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methylpyrimidin-2-ylmethyl)amino]methyl}piperidinyl-1-yl)methanone (2) by reacting 5-methylpyrimidine-2-methylamine (1) with 1-(4-fluoro-3-chlorobenzoyl)-4-fluoro-4-(hydroxycyanomethyl)piperidine (3). Preparation of (3-chloro-4-fluorophenyl)-...

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Bibliographische Detailangaben
Hauptverfasser: BRUNEL, SERGE, MAUREL, JEAN-LOUIS, VACHER, BERNARD
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Zusammenfassung:Preparation of (3-chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methylpyrimidin-2-ylmethyl)amino]methyl}piperidinyl-1-yl)methanone (2) by reacting 5-methylpyrimidine-2-methylamine (1) with 1-(4-fluoro-3-chlorobenzoyl)-4-fluoro-4-(hydroxycyanomethyl)piperidine (3). Preparation of (3-chloro-4-fluorophenyl)-(4-fluoro-4-{[(5-methylpyrimidin-2-ylmethyl)amino]methyl}piperidinyl-1-yl)methanone (2) by reacting 5-methylpyrimidine-2-methylamine (1) with 1-(4-fluoro-3-chlorobenzoyl)-4-fluoro-4-(hydroxycyanomethyl)piperidine (3). Independent claims are included for the following: (1) 5-methylpyrimidine-2-methylamine (1) as new; and (2) three pyrimidine derivatives of formula (4) as new compounds. one or R 1and R 2H and the other is tert-butoxycarbonyl or benzyloxycarbonyl, or R 1and R 2together complete phthalimido. [Image] ACTIVITY : None given. MECHANISM OF ACTION : 5-Hydroxytryptamine agonist.