- Regio- and stereoselective synthesis of constrained enantiomeric β-amino acid derivatives
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Chlorosulfonyl isocyanate addition to (-)- and (+)-apopinene furnished monoterpene-fused β-lactams in highly regio- and stereospecific reactions. β-Lactams 5 and 13 exhibited reactivities similar to those of the cycloalkane-fused analogs and were easily c
- Szakonyi, Zsolt,Martinek, Tamas A.,Sillanpaeae, Reijo,Fueloep, Ferenc
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experimental part
p. 2296 - 2303
(2009/04/11)
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- CHIRAL CYCLIC ?-AMINO ACIDS AND THEIR DERIVATES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THE USE OF SUCH COMPOUNDS
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The invention relates to chiral cyclic β-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for C1-4 Alk; X stands for -COOH, -CONH2, -CONH(C1-4 Alk), -CON(C1-4 Alk)2, -COO(C1-4 Alk), -COPhe-O-(C1-4 Alk) or -CH2OH; Y stands for -NH2, -NHBoc, -NHFmoc, -NH(C1-4 Alk), -N(C1-4 Alk)2, -NHCH2Ph, or Ar-NH-C(=X0)-N(R0)- wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X + Y stands for -CONH- vagy -CON(Boc)-; with the proviso that when X stands for -COOH, then Y may be only different from -NH2. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.
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Page/Page column 22
(2008/12/05)
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