56829-61-9Relevant academic research and scientific papers
Preparation method of acaricide of fenazaquin
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Paragraph 0025-0026; 0028-0029; 0031-0032; 0034-0035, (2020/09/20)
The invention discloses a preparation method of an acaricide of fenazaquin, and belongs to the field of a pesticide raw drug process. The preparation method is implemented through the following stepsthat (1) 4-tertiary butyl phenethyl alcohol is used as r
Nickel-catalyzed cross-coupling of aryl bromides with tertiary grignard reagents utilizing donor-functionalized N-heterocyclic carbenes (NHCs)
Lohre, Claudia,Droege, Thomas,Wang, Congyang,Glorius, Frank
supporting information; experimental part, p. 6052 - 6055 (2011/06/25)
Metal-catalyzed cross-coupling reactions are among the most important transformations in organic synthesis, allowing the efficient construction of complex structures from simpler, readily available building blocks.Many applications in large and small-scale synthesis can be found in different areas such as agrochemicals, pharmaceuticals and supramolecular chemistry. Whereas the coupling of sp2-hybridized carbon atoms in either reaction partner is well established, the use of CACHTUNGTRENUNG(sp3)-hybridized substrates presents some challenges. Catalytic cross-coupling of sterically hindered tertiary alkyl substrates is especially difficult, generally resulting in low yields, and thus, only few reports exist.[27] A big challenge in this field is not only to get the required level of reactivity, but also to overcome competing pathways like β-hydride elimination, hydrodehalogenation or isomerization
Structure-activity relationships of simplified resiniferatoxin analogues with potent VR1 agonism elucidates an active conformation of RTX for VR1 binding
Lee, Jeewoo,Kim, Su Yeon,Park, Soyoung,Lim, Ju-Ok,Kim, Ji-Min,Kang, Myungshim,Lee, Jiyoun,Kang, Sang-Uk,Choi, Hyun-Kyung,Jin, Mi-Kyung,Welter, Jacqueline D.,Szabo, Tamas,Tran, Richard,Pearce, Larry V.,Toth, Attila,Blumberg, Peter M.
, p. 1055 - 1069 (2007/10/03)
We previously described a series of N-(3-acyloxy-2-benzylpropyl) homovanillate and N′-(4-hydroxy-3-methoxybenzyl) thiourea derivatives that were potent VR1 agonists with high-affinities and excellent analgesic profiles. The design of these simplified RTX analogues was based on our RTX-derived pharmacophore model which incorporates the 4-hydroxy-3- methoxyphenyl (A-region), C20-ester (B-region), orthophenyl (C1-region) and C3-keto (C2-region) groups of RTX. For the purpose of optimizing the spatial arrangement of the four principal pharmacophores on the lead agonists (1-4), we have modified the distances in the parent C-region, 3-acyloxy-2-benzylpropyl groups, by lengthening or shortening one carbon to vary the distances between the pharmacophores. We find that two of the amides, 4 and 19, possess EC50 values i) and calcium influx (EC50) values. The binding affinities of the agonists correlated best with the RMS values derived from RTX conformation E (r2=0.92), predicting a model of the active conformation of RTX and related vanilloids for binding to VR1. Poorer correlation was obtained between any of the conformations and the EC 50 values for calcium influx.
