- Synthesis and evaluation of new 18F-labelled acetamidobenzoxazolone-based radioligands for imaging of the translocator protein (18 kDa, TSPO) in the brain
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The visualization of the activated microglia/TSPO is one of the main aspects of neuroimaging. Here we describe two new 18F-labelled molecules, 2-[5-(4-[18F]fluoroethoxyphenyl)- ([18F]2) and 2-[5-(4-[18F]fluoropr
- Tiwari, Anjani K.,Fujinaga, Masayuki,Yui, Joji,Yamasaki, Tomoteru,Xie, Lin,Kumata, Katsushi,Mishra, Anil K.,Shimoda, Yoko,Hatori, Akiko,Ji, Bin,Ogawa, Masanao,Kawamura, Kazunori,Wang, Feng,Zhang, Ming-Rong
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Read Online
- TRIOXACARCIN-ANTIBODY CONJUGATES AND USES THEREOF
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Provided herein are trioxacarcin-antibody drug conjugates of Formula (I): and pharmaceutically acceptable salts thereof, wherein R7 is -L-B, wherein L is a linking group, and B is an antibody or antibody fragment. Also provided are methods of preparing the antibody-drug conjugates, pharmaceutically acceptable compositions thereof, and methods of their use and treatment. Further provided are precursors to the trioxacarcin- antibody drug conjugates (e.g., compounds of Formula (II), novel trioxacarcins without an antibody conjugated thereto), pharmaceutical compositions thereof, and methods of their use and treatment.
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Paragraph 00474; 00481
(2019/02/25)
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- Synthetic method for cyclopropyl diphenyl sulfonium trifluoromethanesulfonic salt
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The invention provides a synthetic method for cyclopropyl diphenyl sulfonium trifluoromethanesulfonic salt. The synthetic method includes the steps that (a) 3-halogen-1-propyl alcohol and trifluoromethanesulfonic anhydride serve as raw materials for synth
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Paragraph 0029; 0030; 0031; 0032
(2017/08/28)
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- Synthesis of quaternary α-methyl α-amino acids by asymmetric alkylation of pseudoephenamine alaninamide pivaldimine
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The utility of pseudoephenamine as a chiral auxiliary for the alkylative construction of quaternary α-methyl α-amino acids is demonstrated. The method is notable for the high diastereoselectivities of the alkylation reactions, for its versatility with respect to electrophilic substrate partners, and for its mild hydrolysis conditions, which provide α-amino acids without salt contaminants. Alternatively, α-amino esters can be obtained by direct alcoholysis.
- Hugelshofer, Cedric L.,Mellem, Kevin T.,Myers, Andrew G.
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supporting information
p. 3134 - 3137
(2013/07/26)
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- Synthesis and evaluation of novel radioligands for positron emission tomography imaging of metabotropic glutamate receptor subtype 1 (mGluR1) in rodent brain
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We designed three novel positron emission tomography ligands, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-thiazol-2-yl)-4-[ 11C]methoxy-N-methylbenzamide ([11C]6), 4-[ 18F]fluoroethoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methylbenzamide ([18F]7), and 4-[ 18F]fluoropropoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1, 3-thiazol-2-yl]-N-methylbenzamide ([18F]8), for imaging metabotropic glutamate receptor type 1 (mGluR1) in rodent brain. Unlabeled compound 6 was synthesized by benzoylation of 4-pyrimidinyl-2-methylaminothiazole 10, followed by reaction with isopropylamine. Removal of the methyl group in 6 gave phenol precursor 12 for radiosynthesis. Two fluoroalkoxy analogues 7 and 8 were prepared by reacting 12 with tosylates 13 and 14. Radioligands [ 11C]6, [18F]7, and [18F]8 were synthesized by O-[11C]methylation or [18F]fluoroalkylation of 12. Compound 6 showed high in vitro binding affinity for mGluR1, whereas 7 and 8 had weak affinity. Autoradiography using rat brain sections showed that [ 11C]6 binding is aligned with the reported distribution of mGluR1 with high specific binding in the cerebellum and thalamus. PET study with [ 11C]6 in rats showed high brain uptake and a similar distribution pattern to that in autoradiography, indicating the usefulness of [ 11C]6 for imaging brain mGluR1.
- Fujinaga, Masayuki,Yamasaki, Tomoteru,Yui, Joji,Hatori, Akiko,Xie, Lin,Kawamura, Kazunori,Asagawa, Chiharu,Kumata, Katsushi,Yoshida, Yuichiro,Ogawa, Masanao,Nengaki, Nobuki,Fukumura, Toshimitsu,Zhang, Ming-Rong
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scheme or table
p. 2342 - 2352
(2012/05/31)
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- PRODUCTION OF COMPOUNDS COMPRISING CF30 GROUPS
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The present invention relates to a process for the preparation of compounds containing CF3O groups using compounds containing at least one group Y, in which Y=—Hal, —OSO2(CF2)zF, —OSO2CzH2z+1 (z=1-10), —OSO2F, —OSO2Cl, —OC(O)CF3— or —OSO2Ar, to a process for the preparation of compounds containing CF3O groups using KOCF3 and/or RbOCF3, and to novel compounds containing CF3O groups, and to the use thereof.
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Page/Page column 7
(2011/04/24)
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- A new method for the preparation of nitrogen-containingheterocycles using diphenylsulfonium triflates
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Various nitrogen heterocycles were produced by the reactions of ω-bromoalkyldiphenylsulfonium or diphenylsyylsulfonium triflates with nitrogen nucleophiles. Further, the reactions of diphenylstyrylsulfonium triflates with N-metalated phthalimide and imida
- Yamanaka, Hiroyuki,Yamane, Yoshinobu,Mukaiyama, Teruaki
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p. 2813 - 2826
(2007/10/03)
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- ACRIDONE COMPOUNDS
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Novel acridone compounds represented by the general formula (I) or pharmaceutically acceptable salts thereof efficacious in the prevention and treatment of diseases in which chemical transmitters such as histamine and leukotriene participate, typified by
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- Synthesis of N-Substituted Pyrroles From Azlactones via 1,3-Oxazolium 5-Oxides
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In situ N-alkylation of azlactones (1,3-oxazol-5(4H)-ones) with reactive alkylating agents has been successfully accomplished.The resulting mesoionic 1,3-oxazolium 5-oxides (munchnones) are further transformed into N-alkylated pyrroles via a 1,3-dipolar c
- Hershenson, Fred. M.,Pavia, Michael R.
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p. 999 - 1001
(2007/10/02)
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- A Rapid and Efficient Method for the Fluoroalkylation of Amines and Amides. Development of a Method Suitable for Incorporation of the Short-Lived Positron Emitting Radionuclide Fluorine-18
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We have described a two-step method for the preparation of fluoroalkyl-substituted amines and amides.The sequence involves fluoride ion displacement of a haloalkyl trifluoromethanesulfonate (triflate), followed by fluoroalkylation of the heteroatom system (amine or amide) by the fluoroalkyl halide.Alternatively, the fluoroalkyl halide can be prepared by halofluorination of a terminal olefin.These reactions have been used to prepare various fluoroalkyl derivatives of N-phenylpiperazine and N-fluoroalkyl derivatives of the neuroleptic agent spiperone (7).The sequence is rapid, convenient, and efficient, even when fluoride ion is the limiting reagent.Therefore, it is readily adaptable to the preparation of a variety of compounds labeled with the short half-life (t1/2 = 110 min) positron-emitting radionuclide fluorine-18.
- Chi, Dae Yoon,Kilbourn, Michael R.,Katzenellenbogen, John A.,Welch, Michael J.
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p. 658 - 664
(2007/10/02)
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