- Synthesis method of 3, 5-disubstituted 1, 2, 4-oxadiazole
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The invention relates to a novel synthetic method for synthesizing 3, 5-disubstituted-1, 2, 4-oxadiazole, in particular to a synthetic method of 3, 5-disubstituted-1, 2, 4-oxadiazole. The method disclosed by the invention has the characteristics that the reaction is carried out at room temperature, the 1, 2, 4-oxadiazole is synthesized at high yield by a one-pot method, and a final product does not need to be subjected to column chromatography. The 3, 5-disubstituted-1, 2, 4-oxadiazole synthesized by the invention can be used in the field of medical treatment.
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Paragraph 0031-0034
(2021/06/22)
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- Highly efficient one-pot preparation of 1,2,4-oxadiazoles in the presence of diazabicycloundecene
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New highly efficient method for the cyclization of acylamidoximes in the presence of diazabicycloundecene was developed and incorporated into a general and practical one-pot synthesis of 1,2,4-oxadiazoles (11 examples, 85-97% yields).
- Lukin, Kirill,Kishore, Vimal
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p. 256 - 261
(2014/02/14)
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- Synthesis and structure-activity relationships of 3,5-diarylisoxazoles and 3,5-diaryl-1,2,4-oxadiazoles, novel classes of small molecule interleukin-8 (IL-8) receptor antagonists
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A novel series of 3,5-diarylisoxazole and 3,5-diaryl-1,2,4-oxadiazole IL-8 inhibitors has been identified. These compounds exhibit activity in an IL-8 binding assay as well as in a functional assay of IL-8 induced elastase release from neutrophils. In add
- Weidner-Wells, Michele A.,Henninger, Todd C.,Fraga-Spano, Stephanie A.,Boggs, Christine M.,Matheis, Michele,Ritchie, David M.,Argentieri, Dennis C.,Wachter, Michael P.,Hlasta, Dennis J.
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p. 4307 - 4311
(2007/10/03)
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- A preferred synthesis of 1,2,4-oxadiazoles
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An efficient and high-yielding one-pot synthesis of 1,2,4-oxadiazoles from carboxylic acids and amidoximes is described. Activation of the carboxylic acid using hydroxybenzotriazole (HOBt) and EDC/HCl followed by reaction with an amidoxime generates an oxime ester. Without isolation, the oxime ester is dehydrated to give the oxadiazole ring.
- Pipik, Brenda,Ho, Guo-Jie,Williams, J. Michael,Conlon, David A.
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p. 1863 - 1870
(2007/10/03)
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- Parallel synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation
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We describe the synthesis of 1,2,4-oxadiazoles from carboxylic acids and amidoximes using 2-(1H-benzotriazole-1-yl)-1,1,3,3-tetramethyluronium tetrafluoroborate (TBTU) as an activating agent of the carboxylic acid function for the O-acylation step. This method was used for the synthesis of a library of 24 1,2,4-oxadiazoles.
- Poulain, Rébecca F.,Tartar, André L.,Déprez, Benot P.
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p. 1495 - 1498
(2007/10/03)
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- Parallel synthesis of 1,2,4-oxadiazoles using CDI activation
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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 products by simple liquid-liquid extraction and filtration.
- Deegan, Tracy L.,Nitz, Theodore J.,Cebzanov, Diane,Pufko, Denise E.,Porco Jr., John A.
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p. 209 - 212
(2007/10/03)
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