Cleavage of Sulfone Linkers

2 Cleavage of Sulfone Linkers. This section describes the synthesis of V-heterocycles using different sulfone linker cleavage techniques. 

Nucleophilic Displacement. Sulfones can be displaced by a variety of nucleophiles, the most common of which are the amines. Using this cleavage technique, a range of libraries, including pyrimidines, pyrimido[4,5-iflpyrimidines, purines, and triazines, each possessing a diverse variety of amine functionalities, have been prepared. 

9-Trisubstituted Purines. Schultz and Brun have reported a traceless resin capture and release strategy for the solid-phase synthesis of 2,6,9-trisubstituted purines 

3 days, 4-methoxyphenylboronic acid or PdCl2(dppe), Cul, DIEA, 3-methylpentyn-3-ol, 80 C 36 h 

Pyrimidine Derivatives. Lam and coworkers have also published the preparation of 3,4,6-trisubstituted-2-pyridones 49, pyridine-2-thiones, and pyrimidine-2-ones 50 and 

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Scheme 71 Cleavage of sulfone linkers containing /3-carbonyl functionality...

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