71126-73-3Relevant articles and documents
A selective and efficient demesylation using methylmagnesium bromide
Cossy,Ranaivosata,Bellosta,Wietzke
, p. 3109 - 3112 (1995)
The chemoselective regeneration of alcohols from mesylates was accomplished by using methylmagnesium bromide in THF.
Composition for controlling pine wood nematode containing benzyloxyalcohol
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Paragraph 0055-0056, (2021/06/15)
The present invention relates to a composition for controlling pine nematode comprising a benzyloxyalcohol compound and a method for controlling pine nematode using the same.
Stereoselective total synthesis of siladenoserinols A and D
Liu, Yinxin,Liu, Jun,Zhao, Chuanfang,Du, Yuguo
supporting information, p. 3264 - 3268 (2021/05/04)
The stereoselective total synthesis of siladenoserinols A and D has been accomplished using carbohydrate as a chiral template. The feature of this work is to build the medicinally privileged 6,8-DOBCO scaffold through a cascade reaction of hydrogenation/deacetalization/ketalization in a one-pot process, that is, to take advantage of a thermodynamically controlled bicyclization of polyhydroxyketone under HCl/MeOH reaction conditions. The current cost-effective synthetic strategy could facilitate the bioactivity investigation of siladenoserinols.
Nematicidal activity of benzyloxyalkanols against pine wood nematode
Kim, Junheon,Lee, Su Jin,Park, Joon Oh,Yoon, Kyungjae Andrew
, p. 1 - 9 (2021/03/15)
Pine wilt disease (PWD) is caused by the pine wood nematode (PWN; Bursaphelenchus xylophilus) and causes severe environmental damage to global pine forest ecosystems. The current strategies used to control PWN are mainly chemical treatments. However, the continuous use of these reagents could result in the development of pesticide-resistant nematodes. Therefore, the present study was undertaken to find potential alternatives to the currently used PWN control agents abamectin and emamectin. Benzyloxyalkanols (BzOROH; R = C2–C9 ) were synthesized and the nematicidal activity of the synthetic compounds was investigated. Enzymatic inhibitory assays (acetylcholinesterase (AChE) and glutathione S-transferase (GST)) were performed with BzOC8OH and BzOC9OH to understand their mode of action. The benzyloxyalkanols showed higher nematicidal activity than did benzyl alcohol. Among the tested BzOROHs, BzC8OH and BzC9OH showed the strongest nematicidal activity. The LD50 values of BzC8OH and BzC9OH were 246.1 and 158.0 ppm, respectively. No enzyme inhibitory activity was observed for BzC8OH and BzC9OH. The results suggested that benzyloxyalcohols could be an alternative nematicidal agent.
Chemoselective Oxidation of p-Methoxybenzyl Ethers by an Electronically Tuned Nitroxyl Radical Catalyst
Hamada, Shohei,Sugimoto, Koichi,Elboray, Elghareeb E.,Kawabata, Takeo,Furuta, Takumi
supporting information, p. 5486 - 5490 (2020/07/24)
The oxidation of p-methoxy benzyl (PMB) ethers was achieved using nitroxyl radical catalyst 1, which contains electron-withdrawing ester groups adjacent to the nitroxyl group. The oxidative deprotection of the PMB moieties on the hydroxy groups was observed upon treatment of 1 with 1 equiv of the co-oxidant phenyl iodonium bis(trifluoroacetate) (PIFA). The corresponding carbonyl compounds were obtained by treating the PMB-protected alcohols with 1 and an excess of PIFA.
Radiosynthesis of novel N-18F-labeled 18F-FHex-α-l-Glu and 18F-FHex-β-Glu
Wen, Fuhua,Liu, Shaoyu,Ma, Hui,Tang, Ganghua
, p. 222 - 230 (2020/04/02)
N-18F-labeled amino acids are important substitutes for new positron emission tomography (PET) imaging tracers complementing the deficiency of 18F-fluorodeoxyglucose (18F-FDG). In this work, two novel N-6-18F-alkyl amino acid imaging agents, 18F-FHex-α-l-Glu and 18F-FHex-β-Glu, were designed and synthesized as potential probes for PET imaging of tumors. 18F-FHex-α-l-Glu was synthesized using the precursor 6 from 18F-F? with the yield of 16 ± 4% (n = 5, uncorrected) within about 50 minutes. The specific activity was 14.5 GBq/μmol, and the radiochemical purity was more than 95%. 18F-FHex-β-Glu was synthesized using the precursor 12 based on 18F-F? with the yield of 11 ± 3% (n = 3, uncorrected) in about 60 minutes. The specific activity was 9.1 GBq/μmol, and the radiochemical purity was more than 95%.
A MedChem toolbox for cereblon-directed PROTACs
Steinebach, Christian,Sosi?, Izidor,Lindner, Stefanie,Bricelj, Ale?a,Kohl, Franziska,Ng, Yuen Lam Dora,Monschke, Marius,Wagner, Karl G.,Kr?nke, Jan,Gütschow, Michael
supporting information, p. 1037 - 1041 (2019/06/27)
A modular chemistry toolbox was developed for cereblon-directed PROTACs. A variety of linkers was attached to a CRBN ligand via the 4-amino position of pomalidomide. We used linkers of different constitution to modulate physicochemical properties. We equipped one terminus of the linker with a set of functional groups, e.g. protected amines, protected carboxylic acids, alkynes, chloroalkanes, and protected alcohols, all of which are considered to be attractive for PROTAC design. We also highlight different opportunities for the expansion of the medicinal chemists' PROTAC toolbox towards heterobifunctional molecules, e.g. with biotin, fluorescent, hydrophobic and peptide tags.
TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
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Paragraph 1142, (2018/05/24)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
BIPOLAR TETRAETHER LIPIDS
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Paragraph 0423; 0424; 0425, (2017/03/21)
Disclosed herein, inter alia, are compounds, compositions, and liposomes and methods of thereof.
Concise synthesis of hydroxy β -methyl fatty acid ethyl esters
Sakai, Yuki,Asakura, Yukiko,Morita, Mitsuhiro,Takahashi, Takashi
, p. 1195 - 1198 (2017/12/26)
Hydroxy β-methyl fatty acid ethyl esters bearing different carbon chain lengths and varying hydroxyl group positions were successfully synthesized from symmetric diols. These fatty acid derivatives are useful intermediates of chemical probes for metabolic
