Category: 21101-63-3

Kolycheva, M. T. published the artcileFluorinated benzaldehydes in Leuckart and Rodionov reactions, Computed Properties of 21101-63-3, the publication is Zhurnal Organicheskoi Khimii (1989), 25(11), 2367-72, database is CAplus.

Difluoromethylating RCOR¹ [I; R = 2-HOC₆H₄, R¹ = Me; R = 3,4-(HO)₂C₆H₃, R¹ = H] with ClCHF₂ in Me₂CHOH containing KOH at 70° gave 27-82% I [R = 2-CHF₂OC₆H₄, 3,4-(CHF₂O)₂C₆H₃; same R¹]. These and I (R = 2-CF₃C₆H₄, 2- and 4-CHF₂OC₆H₄; R¹ = H) reacted with HCONH₂ at 150-180° to give 57-82% RCHR¹NHCHO, which were hydrolyzed with concentrated HCl in MeOH to give 25-86% RCHR¹NH₂.HCl (II), and reduced with LiAlH₄ in THF to give 30-52% RCH₂NHMe.HCl (R = 4-CHF₂OC₆H₄, 2-CF₃C₆H₄). RCH₂Br (R = 4-CF₃SC₆H₄, 4-C₂F₅OC₆H₄) reacted with urotropine in CHCl₃ and then with aqueous-alc. HCl to give the corresponding II in 25-74% yield. RCHO (R = 2- and 4-CHF₂OC₆H₄) condensed with CH₂(CO₂H)₂ in EtOH containing NH₄OAc to give 40-52% RCH(NH₂)CH₂CO₂H and 18-35% RCH:CHCO₂H. Analogous treatment of PhCOCF₃ gave 56% CF₃CPh(OH)CH₂CO₂H.

Zhurnal Organicheskoi Khimii published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Computed Properties of 21101-63-3.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Dokla, Eman M. E. published the artcileDevelopment of Potent Adenosine Monophosphate Activated Protein Kinase (AMPK) Activators, Product Details of C8H6BrF3S, the publication is ChemMedChem (2015), 10(11), 1915-1923, database is CAplus and MEDLINE.

Previously, the authors reported the identification of a thiazolidinedione-based adenosine monophosphate activated protein kinase (AMPK) activator, compound 1 (N-(4-((3-((1-methylcyclohexyl)methyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenyl)-4-nitro-3-(trifluoromethyl)benzenesulfonamide), which provided a proof of concept to delineate the intricate role of AMPK in regulating oncogenic signaling pathways associated with cell proliferation and epithelial-mesenchymal transition (EMT) in cancer cells. In this study, the authors used compound 1 as a scaffold to conduct lead optimization, which generated a series of derivatives Anal. of the antiproliferative and AMPK-activating activities of individual derivatives revealed a distinct structure-activity relationship and identified 59 (N-(3-nitrophenyl)-N’-(4-((3-((3,5-bis(trifluoromethyl)phenyl)methyl)-2,4-dioxothiazolidin-5-ylidene)methyl)phenyl)urea) as the optimal agent. Relative to 1, compound 59 exhibits multifold higher potency in upregulating AMPK phosphorylation in various cell lines irresp. of their liver kinase B1 (LKB1) functional status, accompanied by parallel changes in the phosphorylation/expression levels of p70S6K, Akt, Foxo3a, and EMT-associated markers. Consistent with its predicted activity against tumors with activated Akt status, orally administered 59 was efficacious in suppressing the growth of phosphatase and tensin homolog (PTEN)-null PC-3 xenograft tumors in nude mice. Together, these findings suggest that 59 has clin. value in therapeutic strategies for PTEN-neg. cancer and warrants continued investigation in this regard.

ChemMedChem published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Product Details of C8H6BrF3S.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary

Kancharla, Papireddy published the artcileLead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials, Recommanded Product: (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, the publication is Journal of Medicinal Chemistry (2020), 63(11), 6179-6202, database is CAplus and MEDLINE.

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clin. available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria. Previously, we described a novel antimalarial acridone chemotype that is potent against both blood-stage and liver-stage malaria parasites. Here, we describe an optimization process that has produced a second-generation acridone series with significant improvements in efficacy, metabolic stability, pharmacokinetics, and safety profiles. These findings highlight the therapeutic potential of dual-stage targeting acridones as novel drug candidates for further preclin. development.

Journal of Medicinal Chemistry published new progress about 21101-63-3. 21101-63-3 belongs to bromides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Bromide,sulfides,Benzyl bromide,Benzene, name is (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane, and the molecular formula is C8H6BrF3S, Recommanded Product: (4-(Bromomethyl)phenyl)(trifluoromethyl)sulfane.

Referemce:
https://en.wikipedia.org/wiki/Bromide,
bromide – Wiktionary