Complex molecules are underrepresented in modern biological screening efforts due to challenges in accessing these types of molecules. Isolation of new natural products is slow, thus, alternative approaches to access natural product like compounds is required. Late stage functionalization is a useful strategy for creating analogues of complex small molecules for structure-activity relationship studies and for creating libraries of structurally complex small molecules. We have developed new strategies based on C-H and C=C bond azidation, as well as C-H bond silyllation, that can be used for late-stage functionalization of natural product derivatives. Azides and silanes obtained from these reactions can be converted into alcohols, amines, amides and triazoles. These C-H bond functionalization strategies and guidelines for their applications toward late-stage complex molecule functionalization will be discussed.<br/>

Late-stage functionalization of complex molecules

253rd National Meeting (2017)

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