19733-68-7Relevant articles and documents
Electron-gain and Electron-loss Centres derived from Chloro Amines
Chandra, Harish,Bathgate, Antoinette,Malpass, John R.,Moss, Richard E.,Symons, Martyn C. R.
, p. 1329 - 1332 (1988)
Exposure of dilute solutions of various dialkyl and cyclic N-chloro amines in trichlorofluoromethane to (60)Co γ-rays at 77 K gave the corresponding cations, R2N.Cl, characterised by (14)N, (35)Cl, and (1)H hyperfine coupling.The results suggest that these radicals are essentially planar at nitrogen, the SOMO being the N-Cl ?* orbital.Similar treatment of dilute solutions in methanol or methyltetrahydrofuran gave the corresponding amino radicals, R2N., also characterised by their e.s.r. spectra.There was no evidence for the formation of the parent radical anions.These results are contrasted with those for N-halogeno imides and the formation of ?* radicals from the cations R3N. and halide ions.
Two-step continuous flow synthesis of amide via oxidative amidation of methylarene
Fang, Zheng,Guo, Kai,He, Wei,Liu, Chengkou,Shi, Tingting,Yang, Yuhang,Yang, Zhao,Zhang, Zhimin
supporting information, (2020/02/28)
A green and efficient method for the synthesis of amides has been developed through oxidative amidation between methylarenes with amines in a two-step continuous flow system. This method integrates methylarene oxidation and amide formation into a single operation which is usually accomplished separately. Oxidation with tert-butyl hydroperoxide (TBHP) as “green” oxidant, the synthesis of amides under mild reaction conditions in continuous flow system and the utilization of methylarenes as starting material make this methodology novel and environment friendly. The practical value of this method is highlighted through the synthesis of high-profile pharmaceutical agents, acetylprocainamide.
Synthesis and application of novel s-guaiazulene sesquiterpenoid alkaloids
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Paragraph 0084; 0085, (2019/08/06)
The invention belongs to the field of synthetic pharmacochemistry and particularly relates to chemical synthesis and an application of a new framework of s-guaiazulene sesquiterpenoid alkaloids from Muriceides collaris. Muriceidine A is successfully designed and synthesized from s-guaiazulene and piperidine acid as raw materials with a chemical method. In order to verify the universality of the synthesis method, azulene aldehyde is linked with piperidine, methylpiperidine, pyrrole, piperidinemethanol, 4-hydroxypiperidine and other N-heterocycle fragments. Screening of antitumor activity in vitro finds that the IC50 values of structure optimized products 2 and 3 for 14 tumor cell strains including 231, MCF-7, K562, HCT-116, Hela, A549, H1975, HUVEC, MGC-803, SH-SY5Y, HO8910, Siha, PC-3 andBEL7402 are smaller than 10 mu M, and therefore, the new framework of s-guaiazulene sesquiterpenoid alkaloids can be used for research and development of antitumor drugs.
Copper-catalyzed one-pot oxidative amidation between methylarenes and amines
Yang, Yuhang,Gu, Jiajia,Fang, Zheng,Yang, Zhao,Wei, Ping,Guo, Kai
, p. 22797 - 22801 (2017/07/10)
A new method for the direct one-pot oxidative amidation between methylarenes and amines catalyzed by copper has been developed. This method integrates methylarene oxidation and amide bond formation, which are usually accomplished separately, into a single operation. In addition, the reaction provides a relatively high yield and has a wide substrate scope. Moreover, the starting reagents are abundant and available in a convenient way at a cheaper price.