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Synthesis and biological evaluation of structurally highly modified analogues of the antimitotic natural product curacin A.
Structure-activity relationship analysis of synthetic analogues of curacin A revealed the lack of activity of traditional heterocyclic replacements of the thiazoline ring or cyclopropyl analogues ofExpand
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Activation of TMSCN by N-heterocyclic carbenes for facile cyanosilylation of carbonyl compounds.
N-Heterocyclic carbenes were found to be highly effective organocatalysts in activating TMSCN for facile cyanosilylation of carbonyl compounds. Cyano transfer from TMSCN to aldehydes and ketonesExpand
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A concise synthesis of butylcycloheptylprodigiosin.
A short and efficient total synthesis of the tripyrrole alkaloid butylcycloheptylprodigiosin is described. Key to the brevity of the approach is a two-step synthesis of macrocyclic formylpyrrole 4Expand
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Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors.
The epidermal growth factor receptor (EGFR), when carrying an activating mutation like del19 or L858R, acts as an oncogenic driver in a subset of lung tumors. While tumor responses to tyrosine kinaseExpand
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Asymmetric synthesis of active pharmaceutical ingredients.
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Organometallic methods for the synthesis and functionalization of azaindoles.
Azaindoles (also called pyrrolopyridines) constitute essential subunits in many pharmaceutically important compounds. The synthesis of azaindoles has been a great synthetic challenge for chemists.Expand
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Copper catalyzed asymmetric propargylation of aldehydes.
The highly enantio- and regioselective copper catalyzed asymmetric propargylation of aldehydes with a propargyl borolane reagent is reported. The methodology demonstrated broad functional groupExpand
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