41018-60-4Relevant academic research and scientific papers
An Investigation of (Diacetoxyiodo)arenes as Precursors for Preparing No-Carrier-Added [18F]Fluoroarenes from Cyclotron-Produced [18F]Fluoride Ion
Haskali, Mohammad B.,Telu, Sanjay,Lee, Yong-Sok,Morse, Cheryl L.,Lu, Shuiyu,Pike, Victor W.
, p. 297 - 302 (2016/01/15)
Treatment of (diacetoxyiodo)arenes (1a-1u) with cyclotron-produced [18F]fluoride ion rapidly affords no-carrier-added [18F]fluoroarenes (2a-2u) in useful yields and constitutes a new method for converting substituted iodoarenes into substituted [18F]fluoroarenes in just two steps.
IODINE(III)-MEDIATED RADIOFLUORINATION
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, (2015/09/28)
A process for fluorination of aromatic compounds employing iodonium ylides and applicable to radiofluorination using 18F is described. Processes, intermediates, reagents and radiolabelled compounds are described.
Tandem catalytic C(sp3)-H amination/sila-sonogashira-hagihara coupling reactions with iodine reagents
Buendia, Julien,Darses, Benjamin,Dauban, Philippe
supporting information, p. 5697 - 5701 (2015/06/16)
A new tandem C-N and C-C bond-forming reaction has been achieved through RhII/Pd0 catalysis. The sequence first involves an iodine(III) oxidant, then the in situ generated iodine(I) by-product is used as a coupling partner. The overall process demonstrates the synthetic value of iodoarenes produced in trivalent iodine reagent mediated oxidations. I(003) is a double agent: A tandem C-N and C-C bond-forming reaction has been achieved through RhII/Pd0 catalysis. The sequence first involves an iodine(III) oxidant, then the in situ generated iodine(I) by-product is used as a coupling partner. The overall process affords complex building blocks with high yields, and demonstrates the synthetic value of iodoarenes produced in trivalent iodine reagent mediated oxidations.
A Mild and General One-Pot Synthesis of Densely Functionalized Diaryliodonium Salts
Qin, Linlin,Hu, Bao,Neumann, Kiel D.,Linstad, Ethan J.,McCauley, Katelyenn,Veness, Jordan,Kempinger, Jayson J.,DiMagno, Stephen G.
supporting information, p. 5919 - 5924 (2015/09/22)
Diaryliodonium salts are powerful and widely used arylating agents in organic chemistry. Here we report a scalable synthesis of densely functionalized diaryliodonium salts from aryl iodides under mild conditions. This two-step, one-pot process has remarkable functional group tolerance, is compatible with commonly employed acid-labile protective group strategies, avoids heavy metal and transition metal reagents, and provides a direct route to stable precursors to PET imaging agents.
Rapid and efficient radiosyntheses of meta-substituted [ 18F]fluoroarenes from [18F]fluoride ion and diaryliodonium tosylates within a microreactor
Chun, Joong-Hyun,Lu, Shuiyu,Pike, Victor W.
experimental part, p. 4439 - 4447 (2011/10/08)
Effective methods for the introduction of the short-lived positron-emitter fluorine-18 (t1/2 = 109.7 min) at high specific radioactivity into fluoroarenes are valuable for the development of radiotracers for molecular imaging with positron emis
FLUORINATION OF AROMATIC RING SYSTEMS
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Page/Page column 38, (2010/05/13)
This disclosure relates to reagents and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
Improved arene fluorination methodology for I(III) salts
Wang, Bijia,Qin, Linlin,Neumann, Kiel D.,Uppaluri, Shriharsha,Cerny, Ronald L.,DiMagno, Stephen G.
supporting information; experimental part, p. 3352 - 3355 (2010/11/02)
(Equation Presented). The use of low polarity aromatic solvents (benzene or toluene) and/or the removal of inorganic salts results in dramatically improved yields of fluorinated arenes from diaryliodonium salts. This methodology is shown to "scale down" to the conditions used typically for radiotracer synthesis.
4-ARYLOXYQUINOLIN-2(1H)-ONES AS MTOR KINASE AND PI3 KINASE INHIBITORS, FOR USE AS ANTI-CANCER AGENTS
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Page/Page column 60, (2010/04/06)
4-aryloxyquinolin-2(1H)-ones as mtor kinase and PI3 kinase inhibitors, for use as anti-cancer agents. Compounds of the formula I and pharmaceutically acceptable salts thereof, wherein A, B, R1, R2, R3, R4, R5, R6, and R7 are defined as set forth herein are disclosed. Also disclosed are pharmaceutical compositions comprising the compounds of the invention and a pharmaceutically acceptable carrier, methods of making the compounds of the invention and methods of using the compounds for inhibiting mTOR and PI3 kinases and for treating cancers.
Unexpected, drastic effect of triflic acid on oxidative diacetoxylation of iodoarenes by sodium perborate. A facile and efficient one-pot synthesis of (diacetoxyiodo) arenes
Hossain, Md. Delwar,Kitamura, Tsugio
, p. 6984 - 6986 (2007/10/03)
An easy, safe, and effective method for preparing (diacetoxyiodo)arenes from iodoarenes is presented. Addition of trifluoromethanesulfonic acid (triflic acid) as a promoter causes a drastic increase in the yield of (diacetoxyiodo)arenes in the reaction of iodoarenes with sodium perborate. The reaction of the iodoarenes with sodium perborate in acetic acid in the presence of triflic acid at 40-45 °C efficiently generates the corresponding (diacetoxyiodo)arenes in high yields within short time.
Alternative, easy preparation of (diacetoxyiodo)arenes from iodoarenes using potassium peroxodisulfate as the oxidant
Hossain, Md. Delwar,Kitamura, Tsugio
, p. 1932 - 1934 (2007/10/03)
An easy, safe and effective method for preparing (diacetoxyiodo)arenes [ArI(OAc)2], from iodoarenes is presented in this paper, using potassium peroxodisulfate as the oxidant. This procedure avoids the use of high temperature and severe reaction conditions. The reaction of the iodoarenes with potassium peroxodisulfate in acetic acid in the presence of concentrated sulfuric acid or trifluoromethane sulfonic acid at room temperature, efficiently generates the corresponding (diacetoxyiodo)arenes in high yield in a short reaction time. Georg Thieme Verlag Stuttgart.
