Jaro

Synthesis
DOI: 10.1055/a-1874-5283

Flavone and analogues represent an important class of biologically and pharmacologically active substances commonly found in the composition of diverse plants as part of the class of secondary metabolites. Herein, an efficient and regioselective synthetic strategy for the preparation of functionalized flavones is demonstrated through sequential demethylation/6-endo-dig intramolecular cyclization of propyn-1-ones, using catalytic amounts of base in the presence of a thiol, by employing NMP as the solvent. The reactions proceeded smoothly under transition-metal-free and open to air conditions, furnishing the desired six-membered heterocycles in moderate to excellent yields, in short reaction time.
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Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany

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Synthesis
DOI: 10.1055/a-1838-9491

An efficient protocol for the amidation of hydrazide with amine has been developed by utilizing I2 as an oxidant under metal- and base-free conditions at room temperature. N-Acylation products of amines were obtained in good to excellent yields without using toxic reagents. This method is operationally straightforward and tolerates aliphatic/aromatic and primary/secondary amines with different hydrazides.
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Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany

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Synlett
DOI: 10.1055/a-1828-1217

Functionalized cyclic amines are essential structural motifs in synthetic chemistry and pharmaceutical chemistry, and Shono-type oxidation is a well-developed electrochemical approach for the synthesis of α- amines. In sharp contrast, electrochemically driven direct β-C(sp3)–H functionalization of amines has been far proven elusive. Herein, we outline the recent advances in this field and highlight our group’s effort to achieve electrochemical β-C(sp3)–H functionalization assisted by ferrocene as molecular electrocatalyst under mild conditions.1 Introduction2 Case studies of α-Functionalization (Shono-Type Oxidation)3 Electrochemical β-C(sp3)–H Acylation4 Conclusion
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Georg Thieme Verlag KG Rüdigerstraße 14, 70469 Stuttgart, Germany

Article in Thieme eJournals:
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