Stereoselective cyanation of chiral α-amino aldehydes by reaction with Nagata's reagent: a route to enantiopure β-amino-α-hydroxy acids
摘要:
Chiral alpha -dibenzylamino aldehydes react with diethylaluminum cyanide leading to anti-beta -dibenzylamino-alpha -hydroxy-cyanides as the major diastereoisomers in good yields and diastereomeric excesses. Hydrolysis of the nitrile derivatives allows the synthesis of enantiopure beta -amino-alpha -hydroxy acids. (C) 2001 Elsevier Science Ltd. All rights reserved.
Compounds of Formula 1
[Region α]-[Region β]-[Region γ] [Region δ] (I)
which are useful as modulators of chemokine activity. The invention also provides pharmaceutical formulations and methods of treatment using these compounds.
Stereoselective cyanation of chiral α-amino aldehydes by reaction with Nagata's reagent: a route to enantiopure β-amino-α-hydroxy acids
作者:José M. Andrés、Marı́a A. Martı́nez、Rafael Pedrosa、Alfonso Pérez-Encabo
DOI:10.1016/s0957-4166(01)00044-1
日期:2001.2
Chiral alpha -dibenzylamino aldehydes react with diethylaluminum cyanide leading to anti-beta -dibenzylamino-alpha -hydroxy-cyanides as the major diastereoisomers in good yields and diastereomeric excesses. Hydrolysis of the nitrile derivatives allows the synthesis of enantiopure beta -amino-alpha -hydroxy acids. (C) 2001 Elsevier Science Ltd. All rights reserved.
The invention relates to 6,7,8,9-Tetrahydro-3H-imidazo[4,5-h]quinolines of formula 1, in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.