1098339-79-7Relevant articles and documents
Kinetic study of proton-transfer reactions of phenylnitromethanes. Implication for the origin of nitroalkane anomaly
Ando, Kenichi,Shimazu, Yu,Seki, Natsuko,Yamataka, Hiroshi
, p. 3937 - 3945 (2011)
Measurements of rate constants and substituent effects for three important elementary steps of proton-transfer reactions of phenylnitromethane were reported. The Hammett ? values for the deprotonation of ArCH2NO 2 with OH-
Broadening antifungal spectrum and improving metabolic stablity based on a scaffold strategy: Design, synthesis, and evaluation of novel 4-phenyl-4,5-dihydrooxazole derivatives as potent fungistatic and fungicidal reagents
Cheng, Maosheng,Cui, Hengxian,Jiang, Hong,Liu, Lei,Su, Xin,Sun, Yin,Wu, Tianxiao,Yin, Wenbo,Zhang, Yuxin,Zhao, Dongmei,Zhao, Liyu
, (2021/11/11)
5-phenylthiophene derivatives exhibited excellent antifungal activity against Candida albicans, Candida tropicalis and Cryptococcus neoformans. However, optimal compound 7 was inactive against Aspergillus fumigatus and unstable in human liver microsomes in vitro with a half-life of 18.6 min. To discover antifungal agents with a broad spectrum and improve the metabolic properties of the compounds, the scaffold hopping strategy was adopted and a series of 4-phenyl-4,5-dihydrooxazole derivatives were designed and synthesized. It was especially encouraging that compound 22a displayed significant antifungal activities against eight susceptible strains and seven FLC-resistant strains. Furthermore, the potent compound 22a could prevent the formation of fungalbiofilms and displayed satisfactory fungicidal activity. In addition, the metabolic stability of compound 22a was improved significantly, with the half-life of 70.5 min. Compound 22a was almost nontoxic to mammalian A549, MCF-7, HepG2, and 293T cells. Moreover, pharmacokinetic studies in SD rats showed that compound 22a exhibited pharmacokinetic properties with a bioavailability of 15.22% and a half-life of 4.44 h, indicating that compound 22a is worthy of further study.
Method for preparing p-benzaldehyde
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Paragraph 0016; 0034; 0035, (2016/10/10)
The invention discloses a method for preparing trifluoromethylbenzaldehyde. P-trifluoromethyl chlorobenzene, nitromethane and triethylamine are adopted as initial raw materials, an intermediate 1-nitro methyl-4-benzotrifluoride is prepared through a substitution reaction without a solvent or under the condition that a solvent exists, and then the target product trifluoromethylbenzaldehyde is prepared through an oxidizing reaction under the action of ozone. The mass percentage content of obtained trifluoromethylbenzaldehyde ranges from 98.1% to 99.5% (liquid chromatogram, external standard method), and the total yield ranges from 90.3% to 96.5% (by p-trifluoromethyl chlorobenzene). The reaction equation is shown in the specification. According to the method, the synthetic raw materials and the process routine are improved and innovated, no metal catalyst is adopted any more, the raw materials are cheap and easy to obtain, the process procedure and operation are easy, aftertreatment is easy, a high-quality p-benzaldehyde product can be prepared through two popular reaction steps, namely, the substitution reaction and the ozonation reaction, and the reaction yield and product quality are both high.
Scalable, easy synthesis, and efficient isolation of arylnitromethanes: a revival of the Victor Meyer reaction
Alaime, Thibaud,Delots, Audrey,Pasquinet, Eric,Suzenet, Franck,Guillaumet, Gérald
, p. 1337 - 1341 (2017/01/21)
A modified approach to synthesize and isolate arylnitromethanes is described. The method takes advantage of the significant difference in acidity between the arylnitromethane and the major impurity of the reaction, the nitrite ester. The arylnitromethanes resulting from this process are obtained in high yields and are analytically pure, i.e., they do not require distillation or further purification, which is a comfortable improvement of the ancestral Victor Meyer reaction.
