398125-99-0

Upstream product

• 2130-97-4 (S)-N^α-phthaloyl-O-benzyltyrosine 
• 16652-64-5 O-benzyl-S-tyrosine 
• 85-44-9 phthalic anhydride 
• 4376-18-5 Monomethyl phthalate 
• 438470-19-0 methyl 2-(N-succinimidyloxycarbonyl)benzoate 

Downstream Products

• 927426-01-5 C₂₅H₂₀N₄O₃ 
• 927426-07-1 C₂₄H₁₈N₂O₃ 
• 927426-02-6 C₁₇H₁₈N₄O 
• 927426-08-2 C₂₄H₁₉N₅O₃ 
• 927426-09-3 C₁₆H₁₇N₅O 
• 927426-11-7 C₂₅H₂₁N₅O₃ 
• 927426-10-6 C₂₅H₂₁N₅O₃ 

Relevant academic research and scientific papers

Selective Removal of Aminoquinoline Auxiliary by IBX Oxidation

8-Aminoquinoline (AQ) is a widely used bidentate auxiliary in metal-catalyzed directed C-H functionalization reactions. Herein, we report an efficient and chemoselective method to convert various N-quinolyl carboxamides to primary amides with the treatment of a stoichiometric amount of 2-iodoxybenzoic acid oxidant or the combination of a catalytic amount of 2-iodobenzoic acid and Oxone co-oxidant in mixed solvents of H2O and HFIP. Its unique compatibility with the Phth-protected α-amino acid (αAA) substrates enhances the overall synthetic utility of the AQ-directed palladium-catalyzed C-H functionalization strategy for synthesis of complex αAAs.

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.

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.

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.

Rapid procedure for N-phthaloylation of α-amino carboxamides, α-amino alcohols, α-amino esters and dipeptide derivatives

A rapid, one-pot synthesis and mild procedure for the N-phthaloylation of α-amino carboxamides is described. In acetonitrile, these derivatives react with mono-methylphthalate in the presence of BOP and i-Pr2NEt to afford the intermediate Nα-[(o-methoxycarbonyl)benzoyl]amino carboxamides, which undergo rapid cyclization in the presence of aqueous sodium carbonate to afford the corresponding Nα-phthaloylamino carboxamides in excellent yields. The reaction also works efficiently with α-amino esters, α-amino alcohols and dipeptide esters or amides.