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Applications of caged-designed proton sponges in base-catalyzed transformations
Superbasic properties of caged proton sponges (PSs) – substituted diazatetracyclo[4.4.0.13,10.15,8]dodecanes (DTDs) – were utilized in Knoevenagel and Claisen–Schmidt condensations, the PudovikExpand
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An Extended Approach for the Development of Fluorogenic trans‐Cyclooctene–Tetrazine Cycloadditions
Inverse‐electron‐demand Diels–Alder (iEDDA) cycloaddition between 1,2,4,5‐tetrazines and strained dienophiles belongs among the most popular bioconjugation reactions. In addition to its fastExpand
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Substituted diazatetracyclo[4.4.0.1(3,10).1(5,8)]dodecanes as stable caged proton sponges.
Herein, we report a molecular framework design differing significantly from the traditional topology of proton sponges. We developed a synthetic approach to the preparation of caged secondary aminesExpand
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Design and Synthesis of Aza-Bicyclononene Dienophiles for Rapid Fluorogenic Ligations.
Fluorogenic bioorthogonal reactions enable visualization of biomolecules under native conditions with excellent signal-to-noise ratio. Here, we present the design and synthesis ofExpand
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Unexpected Heterocyclic Products from Cycloaddition Reactions of Nonsymmetrical Allenyl Aldoketazines with Substituted Alkynes
Thermally initiated cycloaddition reactions of nonsymmetrical allenyl azines 1 with alkynes or other dipolarophiles usually lead to compounds with three fused, five-membered heterocyclic rings. WithExpand
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Photochemical Formation of Dibenzosilacyclohept-4-yne for Cu-Free Click Chemistry with Azides and 1,2,4,5-Tetrazines.
Photochemical generation of dibenzosilacyclohept-4-yne 3 from the corresponding cyclopropenone 1 and its copper-free click reactions are reported. Steady-state irradiation, kinetic, and transientExpand
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Dihydropyrrolo[1,2-b]pyrazoles: withasomnine and related compounds
In the paper we indicate the increasing importance of derivatives containing a dihydropyrrolo[1,2-b]pyrazole (DPP) core. We try to show our synthetic approach based on an improved Kulinkovich methodExpand
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Bioorthogonal Fluorescence Turn‐On Labeling Based on Bicyclononyne−Tetrazine Cycloaddition Reactions that Form Pyridazine Products
Abstract Fluorogenic bioorthogonal reactions enable visualization of biomolecules with excellent signal‐to‐noise ratio. A bicyclononyne−tetrazine ligation that produces fluorescent pyridazineExpand
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Single-Step Formation of Pyrimido[4,5-d]pyridazines by a Pyrimidine-Tetrazine Tandem Reaction.
A straightforward synthesis of pyrimido[4,5-d]pyridazines from pyrimidines and tetrazines under basic conditions is reported. Deprotonated, substituted 5-halopyrimidines readily react with variouslyExpand
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Application of Pd-Catalyzed Cross-Coupling Reactions in the Synthesis of 5,5-Dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles that Inhibit ALK5 Kinase.
C-H activation of position 3 of a substituted pyrazole ring catalyzed by palladium(II) was straightforward and convenient for arylated or heteroarylatedExpand
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