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2005
Pyridine derivatives
R 0380
Isosteric N-Arylpiperazine Replacements in a Series of Dihydropyridine NPY1
Antagonists. — Aminopiperidines (V) and (IX) are prepared via reductive
15- 131 Receptor
amination with arylpiperidones (IV). This procedure employs ZnCl2 as a Lewis acid in
catalytic amounts. Instead of a stepwise reaction, the reduction by NaBH3CN takes
place in a one-pot procedure, is very fast not very moisture-sensitive and affords high
yields of the desired secondary amines without formation of tertiary amines. In the new
series (VI) and (IX), the aminopiperidine moiety serves as an effective piperazine replacement. Substitution at the ortho position of the phenyl ring is well tolerated for the
binding. Both electron-withdrawing and electron-donating substituents provide very
potent receptor binding in both cyanoguanidine and urea series. — (LUO*, G.;
MATTSON, G. K.; BRUCE, M. A.; WONG, H.; MURPHY, B. J.; LONGHI, D.;
ANTAL-ZIMANYI, I.; POINDEXTER, G. S.; Bioorg. Med. Chem. Lett. 14 (2004)
24, 5975-5978; Dep. Chem., Bristol-Myers Squibb Pharm. Res. Inst., Wallingford, CT
06492, USA; Eng.) — H. Hoennerscheid
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