2,2,2-Trifluoroethyl Chlorooxoacetate—Universal Reagent for One-Pot Parallel Synthesis of N1-Aryl-N2-alkyl-Substituted Oxamides
摘要:
A one-pot parallel synthesis of N-1-aryl-N-2-alkyl-substituted oxamides with 2,2,2-trifluoroethyl chlorooxoacetate was developed. The synthesis of a library of 45 oxamides revealed higher efficiency of this reagent over the known ethyl chlorooxoacetate. The reagent was successfully used to prepare the known oxamide-containing HIV entry inhibitors.
The present invention encompasses compounds of general Formula (1) wherein R
2
, R
3
, Q, W, X, Y and Z are defined as in claim
1
, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
US8207179B2
申请人:——
公开号:US8207179B2
公开(公告)日:2012-06-26
[EN] NEW COMPOUNDS<br/>[FR] NOUVEAUX COMPOSÉS
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2008152014A2
公开(公告)日:2008-12-18
[EN] The present invention encompasses compounds of general Formula (I) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties. [FR] La présente invention concerne des composés représentés par la formule générale (I), dans laquelle R2, R3, Q, W, X, Y et Z désignent des éléments définis dans la revendication 1. Ces composés sont destinés à être utilisés pour le traitement de maladies caractérisées par une prolifération cellulaire excessive ou anormale. L'invention concerne également l'utilisation de ces composés pour la préparation d'un médicament possédant les propriétés décrites ci-dessus.