Category: 660848-57-7

Application In Synthesis of 2-Methoxy-5-(trifluoromethoxy)anilineOn March 23, 2017, Deng, Yonghong; Sun, Cuixiang; Hunt, Diana K.; Fyfe, Corey; Chen, Chi-Li; Grossman, Trudy H.; Sutcliffe, Joyce A.; Xiao, Xiao-Yi published an article in Journal of Medicinal Chemistry. The article was 《Heterocyclyl Tetracyclines. 1. 7-Trifluoromethyl-8-Pyrrolidinyltetracyclines: Potent, Broad Spectrum Antibacterial Agents with Enhanced Activity against Pseudomonas aeruginosa》. The article mentions the following:

Utilizing a total synthesis approach, the first 8-heterocyclyltetracyclines were designed, synthesized, and evaluated against panels of tetracycline- and multidrug-resistant Gram-pos. and Gram-neg. pathogens. Several compounds with balanced, highly potent in vitro activity against a broad range of bacterial isolates were identified through structure-activity relationships (SAR) studies. One compound I demonstrated the best antibacterial activity against Pseudomonas aeruginosa both in vitro and in vivo for tetracyclines reported to date. The experimental part of the paper was very detailed, including the reaction process of 2-Methoxy-5-(trifluoromethoxy)aniline(cas: 660848-57-7Application In Synthesis of 2-Methoxy-5-(trifluoromethoxy)aniline)

2-Methoxy-5-(trifluoromethoxy)aniline(cas: 660848-57-7) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Application In Synthesis of 2-Methoxy-5-(trifluoromethoxy)aniline

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem

Chen, Yen Ting; Seto, Christopher T. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Parallel synthesis of a library of bidentate protein tyrosine phosphatase inhibitors based on the α-ketoacid motif》.Related Products of 660848-57-7 The author mentioned the following in the article:

Protein tyrosine phosphatases (PTPases) regulate intracellular signal transduction pathways by controlling the level of tyrosine phosphorylation in cells. These enzymes play an important role in a variety of diseases including type II diabetes and infection by the bacterium Yersinia pestis, which is the causative agent of bubonic plague. This report describes the synthesis, using parallel solution-phase methods, of a library of 104 potential inhibitors of PTPases. The library members are based on the bis(aryl α-ketocarboxylic acid) motif that incorporates a carboxylic acid on the central benzene linker. This carboxylic acid was coupled with a variety of different aromatic amines through an amide linkage. The aromatic component of the resulting amides is designed to make contacts with residues that surround the active site of the PTPase. The library was screened against the Yersinia PTPase and PTP1B. Based upon the screening results, four members of the library were selected for further study. These four compounds were evaluated against the Yersinia PTPase, PTP1B, TCPTP, CD45, and LAR. Compound 14 has an IC50 value of 590 nM against PTP1B and is a reversible competitive inhibitor. This affinity represents a greater than 120-fold increase in potency over compound 2, the parent structure upon which the library was based. A second inhibitor, compound 12, has an IC50 value of 240 nM against the Yersinia PTPase. In general, the selectivity of the inhibitors for PTP1B was good compared to LAR, but modest when compared to TCPTP and CD45. In addition to this study using 2-Methoxy-5-(trifluoromethoxy)aniline, there are many other studies that have used 2-Methoxy-5-(trifluoromethoxy)aniline(cas: 660848-57-7Related Products of 660848-57-7) was used in this study.

2-Methoxy-5-(trifluoromethoxy)aniline(cas: 660848-57-7) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.Related Products of 660848-57-7

Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem