Tetrahydroquinoline Alkaloid-inspired Chemical Probes

Starting material, we reported the synthesis of four different tricyclic architectures (38-4-1) that were obtained using RCM [29]. For the solid-phase synthesis, compound 42 was obtained from 37 and was successfully loaded onto the alkylsilyl linker-based polystyrene macrobeads, providing 43. In one study, compound 43 was successfully transformed using RCM into the six-membered-ring unsaturated lactam 44. Using this method for library generation remains to be undertaken. 

The conditions for this transformation were highly attractive for developing this method on solid phase. Indeed, this reaction was found to work equally well in 

Alkaloid Natural Product-inspired Small-molecule Binders to Bcl-2 and Bcl-XL and In Silica Studies 

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