Neal D Hone

A HIGHLY ACID LABILE SILICON LINKER FOR SOLID PHASE SYNTHESIS

Abstract A novel arylsilane based linker has been prepared for the solid phase synthesis of small molecule combinatorial libraries. Efficient cleavage is achieved using TFA via anchimerically assisted protiodesilylation to yield aromatic products possessing no residual linker functionality.

Multiple solid-phase synthesis of hydantoins and thiohydantoins

A novel general protocol for the construction of hydantoins and thiohydantoins on a solid support has been developed. Using this novel methodology, the synthesis of a diverse 96-compound library has been achieved. Resin-bound dipeptides are cyclised via the formation of an intermediate isocyanate or isothiocyanate on resin as the key step in the strategy.

Direct release of nitriles from solid phase

Abstract Cleavage conditions are described which allow resin bound secondary amides to be liberated from Sieber or Rink resin as nitriles. The method has been applied to the synthesis of a series of cyanobiaryls.