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Total syntheses and initial evaluation of [Ψ[C(═S)NH]Tpg⁴]vancomycin, [Ψ[C(═NH)NH]Tpg⁴]vancomycin, [Ψ[CH₂NH]Tpg⁴]vancomycin, and their (4-chlorobiphenyl)methyl derivatives: synergistic binding pocket
TLDR
Combined binding pocket and chlorobiphenyl peripherally modified analogues exhibit a remarkable spectrum of antimicrobial activity and impressive potencies against both vancomycin-sensitive and vancomYcin-resistant bacteria.
Convenient and versatile synthesis of formyl-substituted benzoxaboroles
Despite of the medicinal significance of benzoxaboroles, with the newly discovered clinical compound AN2690 as an example, the synthetic method for rapid diversification of this novel scaffold is
Total synthesis of celogentin C by stereoselective C-H activation.
TLDR
A highly stereoselective and efficient synthesis of celogentin C using a novel palladiumcatalyzed C H functionalization strategy and a novel Knoevenagel condensation/radical conjugate addition approach to the Leu-Trp linkage is reported.
Visible-Light-Driven Photocatalytic Initiation of Radical Thiol-Ene Reactions Using Bismuth Oxide.
TLDR
A nontoxic and inexpensive photocatalytic initiation of anti-Markovnikov hydrothiolation of olefins using visible light is reported, enabling a mild and selective method for radical initiation in thiol-ene reactions between a wide scope of oolefins and thiols.
Facile benzo-ring construction via palladium-catalyzed functionalization of unactivated sp3 C-H bonds under mild reaction conditions.
TLDR
A practical synthetic method for the annulation of benzo-rings by the intramolecular coupling of an aryl iodide and a methylene C-H bond is described and an additive of ortho-phenyl benzoic acid functions as a critical ligand for the catalytic process under mild condition, even at near room temperature.
An efficient construction of quinazolin-4(3H)-ones under microwave irradiation
The highly accelerated Niementowski synthesis of quinazolin-4(3H)-one and quinazolin-2,4- dione derivatives under microwave irradiation is reported. Compared to the conventional conditions, this new
Total Synthesis of Mannopeptimycins α and β.
TLDR
The first total synthesis of mannopeptimycin α and β with fully elaborated N- and O-linked sugars is reported, and a gold-catalyzed N-glycosylation of a D- βhEnd substrate with a mannosyl ortho-alkynylbenzoate donor enabled the synthesis of the most challenging N-Man-D-βhEnd unit with excellent efficiency and stereoselectivity.
Total synthesis of the unusual monoterpenoid indole alkaloid (±)-alstilobanine A.
TLDR
The first approach to these alkaloids is described, culminating in a convergent total synthesis of racemic alstilobanine A (3), which lacks the bridging oxepane ring found in 1 and 2, in the same plant.
Enzymatic Glycosylation of Vancomycin Aglycon: Completion of a Total Synthesis of Vancomycin and N- and C-Terminus Substituent Effects of the Aglycon Substrate
Studies on the further development of the sequential glycosylations of the vancomycin aglycon catalyzed by the glycosyltransferases GtfE and GtfD and the observation of unusual, perhaps unexpected,
Total syntheses of the monoterpene indole alkaloids (±)-alstilobanine A and E and (±)-angustilodine.
TLDR
A synthetic strategy has been developed culminating in stereoselective total syntheses of the small class of unusual monoterpenoid indole alkaloids exemplified by alstilobanines A and E and angustilodine, leading to the three alkaloid in racemic form.
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