- Preparation technology for 3-aryl-4-nitro isoxazole compound
-
The invention discloses a preparation technology for a 3-aryl-4-nitro isoxazole compound. The preparation technology comprises the following steps: synthesizing a compound shown as formula II through the nucleophilic addition of hydroxylamine hydrochloride and the compound shown as formula I used as the raw material; acquiring the compound shown as formula III through the substitution reaction of the compound shown as formula II and N-chlorosuccinimide; preparing 1-dimethyl amino-2-nitro ethylene through the reaction of N,N-dimethylformamide dimethyl acetal and nitromethane used as the raw material; and acquiring a target product 3-aryl-4-nitro isoxazole compound through the cyclization reaction of the compound shown as formula III and 1-dimethyl amino-2-nitro ethylene. The raw materials in the synthesis route are low in cost and easily acquired, the operation condition is mild and is easily controlled, the product is easily purified and the preparation technology is a new method for synthesizing the 3-aryl-4-nitro isoxazole compound.
- -
-
Paragraph 0098; 0099
(2018/03/01)
-
- Synthesis of 3,5-Disubstituted isoxazoles containing privileged substructures with a diverse display of polar surface area
-
We designed and synthesized the molecular framework of 3,5-disubstituted isoxazoles containing privileged substructures with various substituents which uniquely display polar surface area in a diverse manner. A library of 3,5-disubstituted isoxazoles were systematically prepared via 1,3-dipolar cycloaddition of alkynes with nitrile oxides prepared by two complementary synthetic routes; method A utilized a halogenating agent with a base and method B utilized a hypervalent iodine reagent. Through the biological evaluation of corresponding isoxazoles via three independent phenotypic assays, the different pattern of biological activities was shown according to the type of privileged substructure and substituent. These results demonstrated the significance of molecular design via introducing privileged substructures and various substituents to make a diverse arrangement of polar surface area within a similar 3-dimensional molecular framework.
- Kim, Mingi,Hwang, Yoon Soo,Cho, Wansang,Park, Seung Bum
-
supporting information
p. 407 - 413
(2017/06/19)
-
- TETRAZOLINONE COMPOUND AND USE THEREOF
-
The compound represented by formula (1): wherein R4 and R5 each represents a hydrogen atom, a halogen atom, or a C1-C3 alkyl group; R6 represents a C1-C4 alkyl group, a C3-C6 cycloalkyl group, or the like; R7, R8, and R9 each represents a hydrogen atom, a halogen atom, or the like; R10 represents a C1-C3 alkyl group, or the like; R13 represents a C1-C3 alkyl group, or the like; and Q represents a phenyl group, or the like; has an excellent control effect on pests.
- -
-
Paragraph 0846
(2015/11/16)
-
- PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF
-
Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient.
- -
-
Paragraph 0073; 0074; 0085; 0086
(2014/02/16)
-
- Synthesis and evaluation o-benzyl oxime-ether derivatives containing ss-methoxyacrylate moiety for insecticidal and fungicidal activities
-
In attempt to lead compounds exhibiting both insecticidal and fungicidal activities, a series of O-benzyl oximeether derivatives were designed and synthesized by introducing ss-methoxyacrylate pharmacophore into a scaffold. The insecticidal activity again
- Hu, Zhi-Bin,Luo, He-An,Wang, Xiao-Guang,Huang, Ming-Zhi,Huang, Lu,Pang, Huai-Lin,Mao, Chun-Hui,Pei, Hui,Huang, Chao-Qun,Liu, Ping-Le,Liu, Ai-Ping
-
p. 1073 - 1076
(2014/05/06)
-
- Facile synthesis of 3-aryl-5-(2-oxopyrrolidin-1-yl)-and 5-(pyridin-4-yl)-4,5-dihydroisoxazoles via 1,3-dipolar cycloaddition under mild conditions
-
A convenient and efficient synthetic approach for the synthesis of 5-substituted 3-aryl-4,5-dihydroisoxazoles is reported. In the presence of triethylamine, a series of hydroximoyl chlorides were transformed into nitrile oxides, followed by reaction with N-vinyl-2-pyrrolidinone (or 4-vinylpyridine) by a 1,3-dipolar cycloaddition to give novel 4,5-dihydroisoxazole derivatives.
- Gong, Yan,Wang, Yong,Zhao, Wen-Tao,Tang, Xiang-Yang
-
p. 499 - 502
(2013/09/12)
-
- Orthogonal aerobic conversion of N-benzyl amidoximes to 1,2,4-oxadiazoles or quinazolinones
-
Concise synthesis of 1,2,4-oxadiazoles was achieved by heating N-benzyl amidoximes with K3PO4 in DMF at 60°C under an O 2 atmosphere via benzylic C-H oxygenation. On the other hand, aerobic treatment of N-benzyl amidoximes
- Zhang, Feng-Lian,Wang, Yi-Feng,Chiba, Shunsuke
-
supporting information
p. 6003 - 6007
(2013/09/12)
-
- PHENYL-ISOXAZOL DERIVATIVES AND PREPARATION PROCESS THEREOF
-
Disclosed are a phenyl-isoxazol derivative compound, which is useful as a treatment material for virus infection, especially, infection of an influenza virus, or its pharmaceutically acceptable derivative, a preparation method thereof, and an illness treatment pharmaceutical composition including the compound as an active ingredient
- -
-
Page/Page column 17
(2012/11/07)
-
- A METHOD OF TREATING LIVER FIBROSIS
-
The present invention relates to a method of treating hepatis C and/or liver fibroisis with 3-cycloalkylaminopyrrolidine derivatives of the present invention
- -
-
Page/Page column 69
(2012/09/11)
-
- Synthesis and biological activity of 3-substituted isoxazolecarboxamides
-
A series of novel 3-substituted isoxazolecarboxamides have been prepared. A key step was 1,3-dipolar cycloaddition of nitrile oxides to α,β-unsaturated esters. Some of these compounds exhibited high fungicidal activities against Alternaria alternata, Botrytis cinerea, Rhizoctonia solani, Fusarium culmorum, and Phytophthora cactorum.
- Gucma, Miroslaw,Golebiewski, W. Marek
-
scheme or table
p. 461 - 469
(2011/07/30)
-
- Concise synthesis and antimicrobial activities of new substituted 5-isoxazolpenicillins
-
The synthesis of a series of new 5-isoxazolpenicillins is described, which were obtained by coupling substituted isoxazoles with 6-APA. Concise large-scale synthesis of 3,5-disubstituted isoxazoles by 1,3-dipolar cycloaddition using copper(I) as catalyst was also investigated. Representative compounds were assayed for antimicrobial activities, showing satisfactory antimicrobial activities against Gram-negative bacteria.
- Wang, Xi-Zhao,Jia, Jiong,Zhang, Yan,Xu, Wei-Ren,Liu, Wei,Shi, Fang-Niu,Wang, Jian-Wu
-
p. 643 - 652
(2008/03/11)
-
- 6-O-substituted erythromycin derivatives having improved gastrointestinal tolerance
-
Compounds having formula (I) are useful for treating bacterial infections while avoiding the concomitant liability of gastrointestinal intolerance. Compositions containing the compounds and methods of treatment using the compounds are also disclosed.
- -
-
Page/Page column 24
(2008/06/13)
-
- Oxadiazoline ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
-
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.
- -
-
Page/Page column 30
(2008/06/13)
-
- Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library
-
In an effort to identify orally bioavailable factor Xa inhibitors, two isoxazolines libraries were prepared to scan for novel P1 ligands. From this work, 4-chloro-3-aniline was identified as a novel and potent benzamidine mimic.
- Lam, Patrick Y. S.,Adams, Jessica J.,Clark, Charles G.,Calhoun, W. Jason,Luettgen, Joseph M.,Knabb, Robert M.,Wexler, Ruth R.
-
p. 1795 - 1799
(2007/10/03)
-