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2004
Pyrazine derivatives
R 0550
Facile Synthesis of 4-Substituted-4-aminopiperidine Derivatives, the Key BuildBlock of Piperazine-Based CCR5 Antagonists. — A new methodology gener46- 156 ing
ates the orthogonally-protected aminopiperidines (V) from the protected isonipecotic
acid (I) with flexible substitution at the 4-position of the piperidine ring. Conversion of
acids (IV) into the key building blocks (V) proceeds smoothly via Curtius rearrangement by a 4-step one-pot procedure. Using methylpiperidinylamine (Va) as a key synthon, the backbone of piperazino-piperidine based CCR5 antagonists can be assembled
in a highly convergent manner via nucleophilic substitution and subsequent lactamization, cf. (VIII)→(IX). The general procedure of preparing structurally diverse piperidino-piperazine amides with building blocks (V) is demonstrated with the convergent
synthesis of the potent CCR5 antagonists (XII). The new method avoids the use of highly toxic and flammable reagents and provides an access to piperazino-piperidine amide
analogues as HIV-1 entry inhibitors. — (JIANG, X.-H.; SONG, Y.-L.; LONG*, Y.-Q.;
Bioorg. Med. Chem. Lett. 14 (2004) 14, 3675-3678; State Key Lab. Drug Res.,
Shanghai Inst. Mater. Med., Chin. Acad. Sci., Shanghai 200031, Peop. Rep. China;
Eng.) — H. Hoennerscheid
2004
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