Parallel synthesis of 1,2,4-oxadiazoles using CDI activation
1999年1月18日 · 1,2,4-Oxadiazoles have been prepared in parallel using 1,1′-carbonyldiimidazole (CDI) as a reagent for both formation and cyclodehydration of O-acyl benzamidoximes. The use of CDI facilitates parallel purification of the oxadiazole …
A new method to synthesize 1,2,4-oxadiazoles by using DMTMM …
2023年7月11日 · The unusual solvent system THF-NMP successfully promoted dehydration process of O-acylated amidoximes and 1,2,4-oxadiazoles were acquired in one-pot. This methodology provides a convenient and facile synthesis of 1,2,4-oxadiazoles with high yield.
Identification of a 1,2,4-Oxadiazole with Potent and Specific …
2023年10月12日 · This oxadiazole displays highly selective, bactericidal killing of Clostridioides (Clostridium) difficile, the bacterium that causes C. difficile infection (CDI) in both hospital and community settings.
A convergent synthesis of 1,3,4-oxadiazoles from acyl hydrazides …
A new approach to 1,3,4-oxadiazoles is described wherein α-bromo nitroalkanes are coupled to acyl hydrazides to deliver the 2,5-disubstituted oxadiazole directly, avoiding a 1,2-diacyl hydrazide intermediate.
The reaction of an amidoxime with an orthoformate19d,22b (Scheme 4) allows access to 5-unsubstituted 1,2,4-oxadiazoles 11, whilst the use of chloroformates, 25 phosgene, thiophos-
Oxadiazoles: moiety to synthesis and utilize | Journal of the …
2021年7月6日 · Efforts were made to simplify the reaction using several activating reagents attached to one oxygen of bisoximes. Neel and Zhao published the synthesis of 1 at a temperature lower than 100 °C using 1,1′-carbonyldiimidazole (CDI) as a dehydrating agent and bisoximes as a reactant [17].
Synthesis and characterization of novel bioactive 1,2,4-oxadiazole ...
2013年10月25日 · Activation of the 4-aminobenzoic acid with CDI and further acylation of the tert-butylamidoxime with DMF as a solvent furnished the O-acylamidoxime, which was not isolated. After heating to 120 °C for four hours, it underwent a cyclodehydration reaction, delivering aniline 1 with 59% yield after purification.
yldiimidazole (CDI) followed by the addition of hydrazine gave the corresponding hydrazides 24a–b.23 As a model, we carried out the reaction of CDI-activated benzoic acid (14b, R1 ¼ Ph) with the leucine-derived hydrazide (24a,R2 ¼ CH 2-CH(CH 3) 2), followed by anin situ dehydration of the disub-stituted hydrazide to yield the corresponding ...
Neel and Zhao published the synthesis of 1. at a temperature lower than 100 °C using 1,1′-carbonyldi-imidazole (CDI) as a dehydrating agent and bisoximes as a reactant [17]. The method showed better functional group toleration at mild reaction conditions.
Synthetic Approaches and Pharmacological Activity of 1,3,4-Oxadiazoles …
2012年8月27日 · The reaction of (N-isocyanimino)triphenylphosphorane with an electron-poor α-haloketone in the presence of aromatic carboxylic acids: A novel three-component reaction for the synthesis of disubstituted 1,3,4-oxadiazole derivatives.