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Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors.
BI-4020 is described, which is a non-covalent, wild-type EGFR sparing, macrocyclic TKI that potently inhibits the above described EGFR variants and induces tumor regressions in a cross-resistant EGFRdel19 T790M C797S xenograft model.
Organometallic methods for the synthesis and functionalization of azaindoles.
In this tutorial review, a survey of the recent development of organometallic chemistry-based methods for azaindole synthesis is surveyed.
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 and tolerate various functional groups.
Efficient Iron‐Catalyzed Kumada Cross‐Coupling Reactions Utilizing Flow Technology under Low Catalyst Loadings
An efficient continuous flow iron-catalyzed Kumada cross-coupling was developed for the coupling of 2-chloropyrazine and various aryl Grignard reagents in presence of low catalyst loadings (0.5
N-heterocyclic carbene-catalyzed silyl enol ether formation.
N-Heterocyclic carbenes (NHCs) were found to catalyze the silyl transfer from trialkylsilyl ketene acetals to ketones. In the presence of a catalytic amount of NHC 3 (IAd, 0.1 to 5 mol %), a series
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 at
Copper-catalyzed annulation of 2-formylazoles with o-aminoiodoarenes.
In the presence of catalytic CuI and sparteine, 2-formylpyrroles can be annulated with o-aminoiodoarenes to give substituted pyrrolo[1,2-a]quinoxalines and related heterocycles. The reaction also
N-heterocyclic carbene catalyzed trifluoromethylation of carbonyl compounds.
Both enolizable and nonenolizable aldehydes and alpha-keto esters undergo facile trifluoromethylation with TMSCF3 at room temperature in the presence of only 0.5-1 mol % of the commercially available NHC, providing CF3-substituted alcohols in good yields.
A Practical Procedure for Reduction of Primary, Secondary and Tertiary Amides to Amines
A mild and general procedure for reduction of primary, secondary, and tertiary amides using catalytic triruthenium dodecacarbonyl and 1,1,3,3-tetramethyldisiloxane as reductant is described. The