Synthesis and Evaluation of Pteroic Acid-Conjugated Nitroheterocyclic Phosphoramidates as Folate Receptor-Targeted Alkylating Agents

2001 ◽  
Vol 44 (1) ◽  
pp. 69-73 ◽  
Author(s):  
Gali Steinberg ◽  
Richard F. Borch
Keyword(s):  
Folate Receptor ◽  
Alkylating Agents ◽  
Pteroic Acid

Targeting the Tumor-Associated Folate Receptor with an111In−DTPA Conjugate of Pteroic Acid

2005 ◽  
Vol 127 (20) ◽  
pp. 7421-7426 ◽  
Author(s):  
Chun-Yen Ke ◽  
Carla J. Mathias ◽  
Mark A. Green
Keyword(s):  
Folate Receptor ◽  
Pteroic Acid

Photocatalytic Alkylation of Pyrroles and Indoles with α-Diazo Esters

2019 ◽  
Author(s):  
Łukasz Ciszewski ◽  
Jakub Durka ◽  
Dorota Gryko
Keyword(s):  
Aromatic Compounds ◽  
Reaction Pathway ◽  
Alkylating Agents ◽  
Catalytic Amount ◽  
Radical Formation ◽  
Reaction Selectivity ◽  
Diazo Esters ◽  
Electron Withdrawing Substituents

This article describes direct photoalkylation of electron-rich aromatic compounds with diazo compoiunds. C-2 alkylated indoles and pyrroles are obtained with good yields even though the photocatalyst (Ru(bpy)3Cl2) loading is as low as 0.075 mol %. For substrates bearing electron-withdrawing substituents the addition of a catalytic amount of N,N-dimethyl-4-methoxyaniline is required. Both EWG-EWG and EWG-EDG substituted diazo esters are suitable as alkylating agents. The reaction selectivity and mechanistic experiments suggest that carbenes/carbenoid intermediates are not involved in the reaction pathway, instead radical formation is proposed.

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