Solution-and Solid-Phase Synthesis of Combinatorial Libraries of Trisubstituted 1,3,5-Triazines. -A general synthesis of the title compounds (III) in solution becomes possible by condensation of amidines or thiouronium salts with (I). The approach can be successfully transferred to the solid phase
Solid phase synthesis of a 1,3,5-trisubstituted pyridinium salt library
โ Scribed by M. Amparo Lago; Thomas T. Nguyen; Pradip Bhatnagar
- Publisher
- Elsevier Science
- Year
- 1998
- Tongue
- French
- Weight
- 199 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0040-4039
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โฆ Synopsis
The synthesis of a 1,3,5-trisubstituted pyridinium salt combinatorial array containing two variable groups was accomplished in good yields. This entailed the incorporation of 5-bromonicotinic acid onto the resin, followed by Pd(0) catalyzed Suzuki coupling, then alkylation of the pyridine nitrogen and finally cleavage from the resin. A mix and split scheme was also carded out.
๐ SIMILAR VOLUMES
The solid phase synthesis of 2,4,5-trisubstituted thiomorpholin-3-ones is described. Starting from a resin-bound protected cysteine, and employing reductive alkylation and amide formation, thiomoq~holin-3one derivatives have been synthesized through intramolecular thioether formation in good yield a
The solid-phase synthesis of trisubsituted guanidines is reported via aza-Wittig coupling of a solid-supported alkyl iminophosphorane with an aryl or alkyl isothiocyanate to generate the corresponding solid-supported carbodiimide which is then reacted with a primary or secondary amine to afford the