A new aminoethyl-polystyrene linker, stable at low concentrations of TFA, has been developed for the solid phase synthesis of peptide amides. The described linker is stable under conditions which remove Bu(t) protecting groups (30-50% TFA in DCM) and the desired product can be finally cleaved off th
Acetophenone-based linker for solid phase synthesis of secondary amides and sulfonamides on the Multipin™ support
✍ Scribed by Chinh T. Bui; Andrew M. Bray; Francesca Ercole; Yen Pham; Firas A. Rasoul; N.Joe Maeji
- Publisher
- Elsevier Science
- Year
- 1999
- Tongue
- French
- Weight
- 225 KB
- Volume
- 40
- Category
- Article
- ISSN
- 0040-4039
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✦ Synopsis
A new and simple linker has been developed for synthesis of secondary amides and sulfonamides. This application is based on the reductive amination reaction between the acetophenone subunit of the linker and a wide range of primary amines including aliphatic and aromatic amines. Cleavage is effected under mild acidic conditions (20% TFA/DCM) to release the products in good yield and purity.
📜 SIMILAR VOLUMES
Methods for the synthesis of chloromethyl and bromomethyl equivalents of Wang's resin are described. To explore the utility of this acid cleavable resin, amines were immobilized through the nitrogen atom, further functionalized, and then cleaved under acid conditions.
## Abstract The incorporation of a specific cleavage site into an oligodeoxynucleotide can be achieved by utilizing the four 5′‐__S__‐(4,4′‐dimethoxytrityl)‐2′‐deoxy‐5′‐thionucleoside 3′‐(2‐cyanoethyl diisopropylphosphoramidites) **5** and **15a**–**c** (__Fig. 1__). Based on the silver ion assiste