1221441-41-3Relevant academic research and scientific papers
Nickel-Catalyzed Reductive Cross-Coupling of Aryl Bromides with Vinyl Acetate in Dimethyl Isosorbide as a Sustainable Solvent
Su, Mincong,Huang, Xia,Lei, Chuanhu,Jin, Jian
supporting information, p. 354 - 358 (2022/01/15)
A nickel-catalyzed reductive cross-coupling has been achieved using (hetero)aryl bromides and vinyl acetate as the coupling partners. This mild, applicable method provides a reliable access to a variety of vinyl arenes, heteroarenes, and benzoheterocycles, which should expand the chemical space of precursors to fine chemicals and polymers. Importantly, a sustainable solvent, dimethyl isosorbide, is used, making this protocol more attractive from the point of view of green chemistry.
Combining photoredox and silver catalysis for azidotrifluoromethoxylation of styrenes
Cong, Fei,Wei, Yongliang,Tang, Pingping
supporting information, p. 4473 - 4476 (2018/05/03)
The first example of an azidotrifluoromethoxylation of styrenes has been achieved by synergistic visible-light-mediated photoredox and silver catalysis. Trifluoromethyl arylsulfonate (TFMS) and the Zhdankin reagent were used as the trifluoromethoxylation reagent and the azide source, respectively. A good functional group tolerance and mild reaction conditions of this method are applicable to late-stage azidotrifluoromethoxylation of complex small molecules. Furthermore, the mechanistic investigations indicate the single-electron transfer involved in the reaction.
Bromotrifluoromethoxy compound and synthetic method thereof
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Paragraph 0097; 0099, (2017/08/27)
According to the invention, a series of trifluoromethoxy reagent precursors are synthesized, and trifluoromethoxy silver with high activity can be obtained under the condition of an activating reagent. By the utilization of the idea, a bromotrifluorometho
UREA DERIVATIVE OR PHARMACOLOGICALLY ACCEPTABLE SALT THEREOF
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Paragraph 0696; 0697; 0698, (2016/12/22)
The present invention provides a urea compound or a pharmacologically acceptable salt thereof that has a formyl peptide receptor like 1 (hereinafter may be abbreviated as FPRL1) agonist effect, a pharmaceutical composition containing the urea compound or the pharmacologically acceptable salt thereof, and a pharmaceutical use thereof. It has been found that a urea derivative represented by the general formula (I) below or a pharmacologically acceptable salt thereof has a superior FPRL1 agonist effect. Compound (I) or a pharmacologically acceptable salt thereof is highly useful for treatment, prevention, or suppression of inflammatory diseases, chronic airway diseases, cancers, septicemia, allergic symptoms, HIV retrovirus infection, circulatory disorders, neuroinflammation, nervous disorders, pains, prion diseases, amyloidosis, immune disorders and the like.
Stabilized 111In-labeled sCCK8 analogues for targeting CCK2-receptor positive tumors: Synthesis and evaluation
Roosenburg, Susan,Laverman, Peter,Joosten, Lieke,Eek, Annemarie,Oyen, Wim J. G.,De Jong, Marion,Rutjes, Floris P. J. T.,Van Delft, Floris L.,Boerman, Otto C.
experimental part, p. 663 - 670 (2011/02/25)
Radiolabeled cholecystokinin-8 (CCK8) peptide analogues can be used for peptide receptor radionuclide imaging and therapy for tumors expressing CCK2/gastrin receptors. Earlier findings indicated that sulfated CCK8 (sCCK8, Asp-Tyr(OSO3H)-Met-Gly-Trp-Met-Asp-Phe-NH2) may have better characteristics for peptide receptor radionuclide therapy (PRRT) than gastrin analogues. However, sCCK8 contains an easily hydrolyzable sulfated tyrosine residue and two methionine residues which are prone to oxidation. Here, we describe the synthesis of stabilized sCCK8 analogues, resistant to hydrolysis and oxidation. Hydrolytic stability was achieved by replacement of the Tyr(OSO3H) moiety by a robust isosteric sulfonate, Phe(p-CH 2SO3H). Replacement of methionine by norleucine (Nle) or homopropargylglycine (HPG) avoided undesired oxidation side-reactions. The phenylalanine analogue Phe(p-CH2SO3H) of l-tyrosine, synthesized by a modification of known synthetic routes, was incorporated in three peptides: sCCK8[Phe2(p-CH2SO3H),Met 3,6], sCCK8[Phe2(p-CH2SO3H),Nle 3,6], and sCCK8[Phe2(p-CH2SO 3H),HPG3,6]. All peptides were N-terminally conjugated with the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-N,N,N,N- tetraacetic acid) and radiolabeled with In-111. In vitro binding assays on CCK2R-expressing HEK293 cells revealed that all three peptides showed specific binding and receptor-mediated internalization, with binding affinity values (IC50) in the nanomolar range. In vitro oxidation studies demonstrated that peptides with Nle or HPG indeed were resistant to oxidation. In vivo targeting studies in mice with AR42J tumors showed that tumor uptake was highest for 111In-DOTA-sCCK8 and 111In-DOTA- sCCK8[Phe2(p-CH2SO3H),Nle3,6] (4.78 ± 0.64 and 4.54 ± 1.15%ID/g, respectively, 2 h p.i.). The peptide with the methionine residues replaced by norleucine (111In-DOTA- sCCK8[Phe2(p-CH2SO3H), Nle3,6]) showed promising in vivo characteristics and will be further investigated for radionuclide imaging and therapy of CCK2R-expressing tumors.
