- Synthesis of ArCF2X and [18F]Ar-CF3via Cleavage of the Trifluoromethylsulfonyl Group
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A versatile synthesis of ArCF2X and [18F]Ar-CF3 type compounds from readily available ArCF2SO2CF3 has been developed. Diverse nucleophiles, including weak nucleophiles such as halides (18F-, Cl-, Br-, and I-), RSH, and ROH, could react with ArCF2SO2CF3 efficiently to give the corresponding difluoromethylene products. The control experiments and the Hammett plot indicated that the reaction might proceed through a difluorocarbocation intermediate generated from the steric hindrance-assisted cleavage of the trifluoromethylsulfonyl group.
- Yang, Ren-Yin,Gao, Xinyan,Gong, Kehao,Wang, Juan,Zeng, Xiaojun,Wang, Mingwei,Han, Junbin,Xu, Bo
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supporting information
p. 164 - 168
(2021/12/17)
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- Medical radioactive isotope labeled P2X7 receptor targeting probe precursor
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The invention relates to the field of organic synthesis, in particular to a medical radioisotope labeled P2X7 receptor targeted probe precursor. The structural formula of the targeted probe precursor is shown as a formula (I) in the specification, X is se
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Paragraph 0078-0082
(2021/08/28)
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- Palladium-catalyzed intramolecular C-H arylation of 2-halo-: N -Boc- N -arylbenzamides for the synthesis of N-H phenanthridinones
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A palladium catalyzed synthesis of N-H phenanthridinones was developed via C-H arylation. The protocol gives phenanthridinones regioselectively by one-pot reaction without deprotection. It exhibits broad substrate scope and affords targets in up to 95% yields. Importantly, it could be applied for the less reactive o-chlorobenzamides.
- Hu, Quan-Fang,Gao, Tian-Tao,Shi, Yao-Jie,Lei, Qian,Yu, Luo-Ting
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p. 13879 - 13890
(2018/04/25)
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- PYRROLIDINE SUBSTITUTED FLAVONES FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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The present invention relates to the use of a compound of formula 1, a stereoisomer or a tautomer thereof, or a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, for the treatment of an inflammatory disorder. The invention further relates to a pharmaceutical composition comprising a compound of formula 1 and at least one pharmaceutically acceptable carrier, for use in the treatment of an inflammatory disorder. The invention also relates to a method for the treatment of an inflammatory disorder by administering a therapeutically effective amount of the compound of formula 1 to a subject in need thereof.
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Page/Page column 35
(2011/09/30)
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- Palladium-catalyzed annulation of haloanilines and halobenzamides using norbornadiene as an acetylene synthon: A route to functionalized indolines, isoquinolinones, and indoles
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A general procedure for the palladium-catalyzed annulation of substituted haloanilines with norbornadiene gives functionalized indolines in 51-98% yield. These indolines can be rapidly converted to benzenoid- substituted indoles and tricyclic indolines. Extension to the use of substituted halobenzamides gives functionalized isoquinolinones in up to 86% yield.
- Thansandote, Praew,Hulcoop, David G.,Langer, Michael,Lautens, Mark
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supporting information; experimental part
p. 1673 - 1678
(2009/07/17)
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- Mitotic kinesin inhibitors
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The present invention relates to 2,3-diarylquinazolinone compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to com
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Page/Page column 26
(2010/11/26)
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- N-PYRROLIDIN-3-YL-AMIDE DERIVATIVES AS SEROTONIN AND NORADRENALINE RE-UPTAKE INHIBITORS
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A compound of Formula (I) and pharmaceutically and/or veterinarily acceptable derivatives thereof, wherein R1 is H, C1_6alkyl, -C(X)Y, C3_8cycloalkyl, aryl, het, aryl-Cl_4alkyl o
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- 3-aroylbenzylpyridazinone derivatives
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Compounds of formula I: STR1 where: R10 is a group represented by formula (A), (B), or (C): STR2 and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.
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- 6-Benzyl-2H-pyridazin-3-one derivatives,their preparation and their use as inhibitors of prostaglandin G/H synthase I and II (COX I and COX II)
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Compounds of formula I: where: the dashed line denotes an optional bond; R1is H, halo, alkyl, alkyloxy, amino, alkylamino, dialkylamino, or acylamino; R3and R4are independently H, halo, alkyl, alkyloxy, or hydroxy; R5
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- Benzylated 1,2,3-triazoles as anticoccidiostats
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Substituted 5-amino-4-carbamoyl-1,2,3-triazoles 3a-w were prepared by two synthetic schemes and evaluated in vivo for anticoccidial activity. Both schemes proceeded by brominating appropriately substituted toluenes 4a-s,v to 5a-s,v. In Scheme I, the brominated benzyl analogues 5 were converted to the corresponding benzyl azides 6, which were treated with cyanoacetamide to yield 1-substituted-5-amino-4-carbamoyl-1,2,3-triazoles 3. In Scheme II, the benzyl halides 5 were employed to alkylate the sodium salt of 5-amino-4-carbamoyl-1,2,3-triazole (7). Preliminary screening data against Eimeria acervulina and E. tenella in chickens suggested structural requirements for maximizing activity. Further evaluation against a relatively resistant series of eight Eimeria field isolates revealed L-651,582 (3a) to be a highly effective coccidiostat. However, unacceptable tissue residues precluded further development. Mechanistic studies on this series of 5-amino-4-carbamoyl-1,2,3-triazoles and, in particular, on L-651,582 (3a) revealed that its mode of action does not involve inhibition of IMP dehydrogenase, but probably interferes with host cell calcium entry. In addition, L-651,582 has been found to have antiproliferative activity in several disease models and was recently reported to possess antimetastatic activity in a model of ovarian cancer progression.
- Bochis,Chabala,Harris,Peterson,Barash,Beattie,Brown,Graham,Waksmunski,Tischler,Joshua,Smith,Colwell,Wyvratt Jr.,Fisher,Tamas,Nicolich,Schleim,Wilks
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p. 2843 - 2852
(2007/10/02)
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