- Palladium-Catalysed C(sp3)?H Glycosylation for the Synthesis of C-Alkyl Glycoamino Acids
-
We have developed a highly efficient and practical approach for palladium-catalyzed trifluoroacetate-promoted N-quinolylcarboxamide-directed glycosylation of inert β-C(sp3)?H bonds of N-phthaloyl α-amino acids with glycals under mild conditions. For the first time, C(sp3)?H activation for glycosylation was achieved to build C-alkyl glycosides. This method facilitates the synthesis of various β-substituted C-alkyl glycoamino acids and offers a tool for glycopeptide synthesis.
- Liu, Yichu,Wang, Yibing,Dai, Wenhao,Huang, Wei,Li, Yingxia,Liu, Hong
-
-
Read Online
- NOVEL HIGH AFFINITY QUINOLINE-BASED KINASE LIGANDS
-
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
- -
-
Paragraph 0244
(2014/01/09)
-
- Novel high affinity quinoline-based kinase ligands
-
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
- -
-
Page/Page column 96
(2008/06/13)
-
- The synthesis of some chiral 2-aminoalkyloxazole-5-carboxylates from isoxazol-5(2H)-ones
-
Ethyl 5-oxo-2,5-dihydroisoxazole-4-carboxylates have been N-acylated by a number of natural and synthetic phthalimidylamino acids in the presence of carbodiimides. The N-acylated products form the corresponding 2-aminoalkyloxazole-5-carboxylates smoothly when irradiated at 300 nm in acetone.
- Cox, Matthew,Prager, Rolf H.,Svensson, Carina E.,Taylor, Max R.
-
p. 897 - 901
(2007/10/03)
-
- Methyl 2-((succinimidooxy)carbonyl)benzoate (MSB): a new, efficient reagent for N-phthaloylation of amino acid and peptide derivatives.
-
A new, efficient, and readily available reagent, methyl 2-((succinimidooxy)carbonyl)benzoate (MSB), for N-phthaloylation of amino acids and amino acid derivatives is described. The phthaloylation procedure is simple and racemization-free and gives excellent results with alpha-amino acids, alpha-amino alcohols, dipeptides, alpha-amino carboxamides, and alpha-amino esters.
- Casimir, J Richard,Guichard, Gilles,Briand, Jean-Paul
-
p. 3764 - 3768
(2007/10/03)
-