Deazapurine Solid-Phase Synthesis:  Combinatorial Synthesis of a Library of N3,N5,C6-Trisubstituted Pyrrolo[3,2-d]pyrimidine Derivatives on Cross-Linked Polystyrene Bearing a Cysteamine Linker

2005 ◽  
Vol 7 (6) ◽  
pp. 977-986 ◽  
Author(s):  
Gil Fridkin ◽  
William D. Lubell
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Combinatorial Synthesis ◽  
Pyrimidine Derivatives ◽  
Phase Synthesis

Combinatorial Synthesis of Exohedrally Modified Fullerene Derivatives

2003 ◽  
Vol 17 (08n09) ◽  
pp. 1910-1915 ◽  
Author(s):  
Yasuhiko Kawamura ◽  
Yasuyuki Akai ◽  
Masao Tsukayama
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Combinatorial Synthesis ◽  
Environmentally Benign ◽  
Azomethine Ylide ◽  
Dipolar Cycloaddition ◽  
Compound Library ◽  
Phase Synthesis ◽  
Fullerene Derivatives ◽  
Wide Range

Fulleropyrrolidines have been very welcomed in a community of a fullerene science. But sometimes the synthesis ends up with disappointing yields of the products. In order to overcome the problem and to explore more environmentally benign method for synthesizing fullerene derivatives having various attachment on the surface of the fullerenes, a solid-phase synthesis is examined. We found that the dipolar cycloaddition of an azomethine ylide, i.e., 2-phenyl-N-benzylideneglycine methyl ester, supported on a Wang resin, proceeded feasibly with C 60 and the objective fulleropyrrolidines were afforded in good yields (>75%). The method is expected to be utilized with wide range of application and it is therefore able to provide a compound library of modified fullerenes which is hard to obtain by other methods employed so far.

Solid-Phase Synthesis and Inhibitory Effects of Some Pyrido[1,2-c]pyrimidine Derivatives on Leukocyte Functions and Experimental Inflammation

2001 ◽  
Vol 44 (6) ◽  
pp. 1011-1014 ◽  
Author(s):  
Pedro Molina ◽  
Enrique Aller ◽  
Ángeles Lorenzo ◽  
Pablo López-Cremades ◽  
Inmaculada Rioja ◽  
...  
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Inhibitory Effects ◽  
Pyrimidine Derivatives ◽  
Phase Synthesis ◽  
Experimental Inflammation

Solid-Phase Traceless Synthesis of Selected Nitrogen-Containing Heterocyclic Compounds. The Encore Technique for Directed Sorting of Modular Solid Support

2001 ◽  
Vol 66 (7) ◽  
pp. 1078-1106 ◽  
Author(s):  
Viktor Krchňák ◽  
Jennifer Smith ◽  
Josef Vágner
Keyword(s):  
Drug Discovery ◽  
Hydrogen Atom ◽  
Heterocyclic Compounds ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Solid Support ◽  
Combinatorial Synthesis ◽  
Target Compound ◽  
Phase Synthesis ◽  
Acidic Reagent

The acid lability of electron-rich N-benzylanilines has been exploited in a linker for the traceless solid-phase synthesis of benzimidazoles, 2-aminobenzimidazoles, quinoxalinones and tetrahydroquinoxalines. The target compound precursors were assembled on a solid-phase support derivatized with either a benzylamine or a benzhydrylamine linker. Exposure to an acidic reagent caused cleavage of the C(benzyl)-N(aniline) bond, releasing the product with only a hydrogen atom on the descending nitrogen. The Encore technique for directed sorting on SynPhase Lanterns has been developed and applied to combinatorial synthesis of generic drug discovery libraries.

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