- [18F]FMDAA1106 and [18F]FEDAA1106: two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR).
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We synthesized and evaluated N-(5-fluoro-2-phenoxyphenyl)-N-(2-[(18)F]fluoromethyl-5-methoxybenzyl)acetamide ([(18)F]-FMDAA1106) and N-(5-fluoro-2-phenoxyphenyl)-N-(2-[(18)F]fluoroethyl-5-methoxybenzyl)acetamide ([(18)F]FEDAA1106) as two potent radioligan
- Zhang, Ming Rong,Maeda, Jun,Furutsuka, Kenji,Yoshida, Yuichiro,Ogawa, Masanao,Suhara, Tetsuya,Suzuki, Kazutoshi
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- Bunte Salt CH2FSSO3Na: An Efficient and Odorless Reagent for Monofluoromethylthiolation
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A practical and efficient monofluoromethylthiolation that employs the typical Bunte salt, sodium S-(fluoromethyl) sulfurothioate, as the sulfur source is described. This reagent reacts readily with a variety of aryl amines and aryl thiols. The high tolerance of functional groups demonstrates the potential of this reaction. In addition, this method is suitable for the late-stage monofluoromethylthiolation of complex bioactive molecules.
- Liu, Fanmin,Jiang, Lvqi,Qiu, Huangyao,Yi, Wenbin
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supporting information
p. 6270 - 6273
(2018/09/27)
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- Direct Monofluoromethylthiolation with S-(Fluoromethyl) Benzenesulfonothioate
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An electrophilic shelf-stable monofluoromethylthiolating reagent S-(fluoromethyl) benezenesulfonothioate (1) was developed. In the presence of a copper catalyst, reagent 1 coupled with a variety of aryl boronic acids to give the corresponding monofluoromethylthiolated arenes in high yields. In addition, addition of reagent 1 to alkyl alkenes in the presence of a silver catalyst gave alkyl monofluoromethylthioethers in high yields.
- Zhao, Qunchao,Lu, Long,Shen, Qilong
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supporting information
p. 11575 - 11578
(2017/09/11)
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- Monofluoromethylthiolation reagent, and preparation method, preparative intermediate and application thereof
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The invention discloses a monofluoromethylthiolation reagent, and a preparation method, preparative intermediate and application thereof. Structure of the monofluoromethylthiolation reagent is shown as in formula I that is shown in the description, wherein R1, R2, R3, R4 and R5 are respectively chosen from one or any of H, C1-C6 linear or branched alkyl, C1-C6 linear or branched alkoxy, C1-C6 linear or branched halogenated alkyl, halogen, nitryl, hydroxyl, cyano group and amino independently. Monofluoromethylthio group is introduced into molecules directly, so that compared with indirect introduction methods in the prior art, the method for the monofluoromethylthiolation reagent has the advantages of good safety, high efficiency, low cost, high substrate universality, mild condition and wide application range. The monofluoromethylthiolation reagent successfully realizes bifunctional reaction of inactivated olefin, coupling reaction of arylboronic acid and other reactions, and an important methodology research foundation is provided for medicine, pesticide, material and other fields.
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Paragraph 0176; 0177; 0178
(2017/09/05)
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- Crystal Structure and Spectroscopic Investigation of Bromofluoro- and Fluoroiodomethane
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The solid states of bromofluoromethane (BFM) and fluoroiodomethane (FIM) are characterized by X-ray diffraction analysis and by Raman spectroscopy. The single crystals were obtained by crystallization in situ at low temperature. BFM and FIM crystallize in the space group I2/a and Abm2, respectively. The Raman spectra of both compounds were recorded in different aggregation states and at different temperatures. Quantum chemical calculations and the X-ray diffraction data are considered to describe the noncovalent interactions of both compounds in the solid state. These interactions are discussed in the context of the σ-hole concept.
- Feller, Michael,Lux, Karin,Kornath, Andreas
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p. 5357 - 5362
(2016/01/25)
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- Palladium-Catalyzed Monofluoromethylation of Arylboronic Esters with Fluoromethyl Iodide
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The first palladium-catalyzed direct monofluoromethylation of arylboronic esters to produce monofluoromethyl arenes is reported. The reaction is typically carried out at room temperature within 4 h and has a good functional group tolerance. The monofluoromethylating agent, CH2FI, was readily prepared via a halogen-exchange process.
- Hu, Jingyu,Gao, Bing,Li, Lingchun,Ni, Chuanfa,Hu, Jinbo
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p. 3086 - 3089
(2015/06/30)
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