Solid-phase synthesis validation

Brohm, D., Metzger, S., Bhargava, A., Muller, O., Lieb, F., and Waldmann, H. (2002) Natural products are biologically validated starting points in structural space for compound library development solid phase synthesis of dysidiolide-derived phosphatase inhibitors. Angew. Chem. Int. Ed. 41, 307-311. 

Validation of Solid-Phase Synthesis and Optimization of Reaction Conditions... 

As of today, apart from straightforward one-step derivatizations, the vast majority of analoging procedures by combinatorial synthesis are carried out on solid support. This overview focuses on organic chemistry adapted to the operation mode of solid-phase synthesis. The translation of protocols from solution chemistry to validated solid-phase procedures is a nontrivial task, often... 

In this chapter several examples were used in the validation of chemistry and precursors. They illustrate the importance of FTIR and color tests in aiding the development of solid-phase chemistry in the loading, diversification, and cleaving steps in combinatorial synthesis. The combined method provides crucial information on reactions carried out on solid supports and offers a fast way to monitor a range of reactions without the need to cleave the compound from resin at intermediate steps. Building block reactivity for similar reactions can also be achieved to guide future synthesis development, as these data may prove powerful for efficient and cost-effective combinatorial library development. 

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