LPCS of small organic molecules

Liquid-phase combinatorial synthesis (LPCS) of small organic molecules 

In the first step, isocyanate 119 was attached to the support affording urethane derivative 120. Subsequent treatment with 6 different amines furnished the corresponding polymer-bound sulfonamides 121. Basic hydrolysis released analytically pure products 122 in high overall yields (95-97%) and purities. Reactions were monitored by NMR spectroscopy. 

Multigeneration assembly strategies with single functional group liberation 

Benzimidazoles are an interesting class of heterocycles which are incorporated into several therapeutic agents. There are several standard preparations of benzimidazoles, but many of them require high temperatures and strong acidic reaction conditions. In general, when adapting a solution-phase methodology into a solid-phase approach, very drastic conditions are to be avoided due to potential problems associated with the stability of the solid support. These criteria were taken into account by Philips and Wei in their approach towards the solid-phase synthesis of a benz-imidazole library.  

Reagents and conditions i) KHMDS, DMF ii) BujSnH, Pd(PPh3)4 iii) DIG. HOBt ( 90% loading level) 

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