Amino Acid;
One Pot Synthesis;
Morpholin-2-one;
Three Component Reaction;
Dibromoethane;
ALPHA-AMINO-ACIDS;
NK1 RECEPTOR ANTAGONIST;
N-HETEROCYCLES;
STEREOSELECTIVE-SYNTHESIS;
PROTEASE INHIBITORS;
CONVERGENT APPROACH;
MULTISTEP SYNTHESIS;
DERIVATIVES;
APREPITANT;
STRATEGY;
D O I:
10.3987/COM-10-S(E)14
中图分类号:
O62 [有机化学];
学科分类号:
070303 ;
081704 ;
摘要:
A new one pot synthetic method to construct 3-substituted morpholine-2-one derivatives is presented. Amino acids refluxed with 1,2-dibromoethane and potassium carbonate in acetonitrile followed by treatment with benzyl bromide in same pot furnished the 3-substituted N-benzyl-morpholine-2-ones in good yields. The simplicity of the reaction conditions and versatility of resulted scaffold to generate wide variety of molecules makes this method more attractive for synthetic organic chemists.