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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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Room temperature palladium-catalyzed cross coupling of aryltrimethylammonium triflates with aryl Grignard reagents.
Aryltrimethylammonium triflates and tetrafluoroborates were found to be highly reactive electrophiles in the Pd-catalyzed cross coupling with aryl Grignard reagents. The coupling reactions proceed atExpand
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Efficient asymmetric synthesis of P-chiral phosphine oxides via properly designed and activated benzoxazaphosphinine-2-oxide agents.
A general, efficient, and highly diastereoselective method for the synthesis of structurally and sterically diverse P-chiral phosphine oxides was developed. The method relies on sequentialExpand
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N-heterocyclic carbene catalyzed trifluoromethylation of carbonyl compounds.
[reaction: see text]. A novel N-heterocyclic carbene (NHC) catalyzed trifluoromethylation reaction of carbonyl compounds was discovered. Both enolizable and nonenolizable aldehydes and alpha-ketoExpand
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N-heterocyclic carbene-catalyzed Mukaiyama aldol reactions.
N-Heterocyclic carbenes were shown to be highly effective catalysts to promote Mukaiyama aldol reactions. In the presence of only 0.5 mol % of N-heterocyclic carbene (5), various aldehydes andExpand
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