Application of an almost traceless linker in the synthesis of 2-alkylthiobenzimidazole combinatorial libraries

  title={Application of an almost traceless linker in the synthesis of 2-alkylthiobenzimidazole combinatorial libraries},
  author={Rachel M. Slade and Ma Phillips and Joel G. Berger},
  journal={Molecular Diversity},
Resin-bound triphenylphosphine was coupledto 4-fluoro-3-nitrobenzyl bromide, and2-alkylthiobenzimidazoles were synthesized onresin in 4 steps using standard chemistries. Cleavage of the compounds from the resin wasachieved with 10% NaOH in MeOH to leave amethyl group at the attachment point. A totalof 47 amines and 40 electrophiles wereevaluated, defining the scope of the reactions,culminating in the synthesis of an 80-membertest library of high purity as determined by HPLC. 
Microwave‐Assisted Solid‐Phase Synthesis of a 1,2‐Disubstituted Benzimidazole Library by Using a Phosphonium Linker
An efficient and rapid microwave-assisted solid-phase method for the synthesis of 5-methyl-1,2-disubstituted benzimidazoles derivatives has been developed. The phosphonium linker, obtained by
Traceless Solid-Phase Synthesis of Ketones via Acid-Labile Enol Ethers: Application in the Synthesis of Natural Products and Derivatives
The use of Wang resin is reported for the traceless synthesis of ketones via acid-labile enol ethers to demonstrate the practicality of this synthetic strategy on the solid-phase synthesis of pyrrolidine-2,4-diones, which represent the core structure of several natural products, including tetramic acid.
Applications of phosphine-functionalised polymers in organic synthesis.
This tutorial review deals with recent advances in the use of phosphine-functionalised polymers in organic synthesis, particularly recyclable catalysts for C-C and C-X bond formation with aryl bromide and chloride substrates.
Synthesis of silicon traceless linker for solid-phase reaction
The synthesized linkers1c and2d could be utilized in constructing a chemical compound library that includes indole, benzodiazepine and phenothiazine (aromatic ring compounds) in solid-phase reactions.
Solid-phase Synthesis of Phosphorus Derivatives
The solid-phase synthesis (SPS) of phosphorus-containing compounds is based mainly on the fact that the chemical process is conducted in a two-phase system. One of the components is connected via
Identification of novel benzimidazole derivatives as anti-Trypanosoma cruzi agents: solid-phase synthesis, structure-activity relationships and molecular docking studies.
The binding orientation of the ligands in the active site of cruzipain provides new guidelines for the further design of better inhibitors, and compound 2a constitute a promising hit compound for novel anti-T.
Multifunctional Linkers for Combinatorial Solid Phase Synthesis
This review covers recent results in the area of multifunctional linkers for solid phase synthesis during the period 2000–2006.


Solid phase synthesis of benzimidazoles
The solid phase synthesis of 3,4-disubstituted-7-carbamoyl-1,2,3,4-tetrahydroquinoxalin-2-ones 8 is described. 4-Fluoro-3-nitrobenzoic acid is tethered to a solid support via the acid group. Aromatic
SNAr-Based Macrocyclization: An Application to the Synthesis of Vancomycin Family Models
The first examples of macrocyclization using the intramol. SNAr reaction are reported. The method has allowed the efficient prepn. of the elusive 16-membered macrocyclic COD and DOE rings related to
Solid phase synthesis of benzimidazolones Solid phase synthesis of benzimidazoles
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An application to the synthesis of vancomycin family models , J
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