- Aromatic C-H amination in hexafluoroisopropanol
-
We report a direct radical aromatic amination reaction that provides unprotected anilines with an improvement in the substrate scope compared to prior art. Hydrogen bonding by the solvent hexafluoroisopropanol to anions of cationic species is responsible for increased reactivity and can rationalize the enhancement in substrate scope. Our findings may have bearings on radical additions to arenes for direct C-H functionalization in general.
- D'Amato, Erica M.,B?rgel, Jonas,Ritter, Tobias
-
p. 2424 - 2428
(2019/02/28)
-
- AMINATION AND HYDROXYLATION OF ARYLMETAL COMPOUNDS
-
In one aspect, the present disclosure provides methods of preparing a primary or secondary amine and hydroxylated aromatic compounds. In some embodiments, the aromatic compound may be unsubstituted, substituted, or contain one or more heteroatoms within the rings of the aromatic compound. The methods described herein may be carried out without the need for transition metal catalysts or harsh reaction conditions.
- -
-
Paragraph 0257
(2018/03/25)
-
- Raltitrexed pharmaceutical composition and preparation method thereof
-
The invention relates to a raltitrexed pharmaceutical composition which is high in safety and a preparation method thereof. The raltitrexed pharmaceutical composition comprises raltitrexed and thiophene related substances, wherein the content of the thiophene related substances is not higher than 0.3%. The raltitrexed pharmaceutical composition is good in safety, effectiveness and stability and can relieve the blood toxicity of the raltitrexed to a certain degree.
- -
-
-
- Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y1 receptor antagonists
-
A novel series of 2-(phenoxyaryl)-3-urea derivatives were designed, synthesized, and biologically evaluated for their anti-thrombotic activity. Most of compounds exhibited good inhibition against P2Y1 receptor. Among them, three compounds 11, 12, and 13 demonstrated good P2Y1 receptor antagonistic potency in vitro (IC50 = 0.62 μM, 0.82 μM, and 0.21 μM, respectively). In antiplatelet aggregation study, four compounds 2, 3, 9, and 13 showed good antiplatelet activity. The possible binding modes of compounds with P2Y1 receptor were also explored by molecular docking simulation. The docking studies demonstrated that compound 13 interacted well with Phe119 through hydrophobic interaction and modestly improved the P2Y1 receptor antagonistic activity, making it justifiable for further investigation.
- Peng, Jingjing,Zhao, Lifen,Wang, Lanlan,Chen, Hui,Qiu, Yunguang,Wang, Jiang,Yang, Huaiyu,Liu, Jun,Liu, Hong
-
p. 302 - 310
(2018/09/18)
-
- Non-deprotonative primary and secondary amination of (hetero)arylmetals
-
Herein we disclose a novel method for the facile transfer of primary (-NH2) and secondary amino groups (-NHR) to heteroaryl-as well as arylcuprates at low temperature without the need for precious metal catalysts, ligands, excess reagents, protecting and/or Erecting groups. This one-pot transformation allows unprecedented functional group tolerance and it is wellsuited for the amination of electron-rich, electron-deficient as well as structurally complex (hetero)arylmetals. In some of the cases, only catalytic amounts of a copper (l) salt is required.
- Zhou, Zhe,Ma, Zhiwei,Behnke, Nicole Erin,Gao, Hongyin,Kürti, László
-
supporting information
p. 115 - 118
(2017/05/16)
-
- Novel acyl hydrazino thiophene derivatives, process for preparing them, their use as medicinal products, pharmaceutical compositions and novel use
-
The invention concerns novel compounds of formula (I), process for making, pharmaceutical compositions and methods of treating diseases associated with abnormal physiological behavior in the secretion and/or the activity of cysteine proteases especially c
- -
-
Page/Page column 20
(2010/02/12)
-
- 2-Aminothiabutadiene as useful building block in the synthesis of 2-aminothiopyrans and 2-aminothiophenes
-
We report a reliable and regiocontrolled alternative route to unsubstituted 2-aminothiopyrans and 2-aminothiophenes. These sulfur heterocycles were prepared by reaction of protected aminothiabutadiene 1 with acrylic dienophiles or acceptor-substituted halomethyl compounds. All compounds were fully characterized by IR, HRMS, and 13C and 1H NMR spectroscopy.
- Robin, Aelig,Meslin, Jean-Claude,Deniaud, David
-
p. 1633 - 1640
(2007/10/03)
-
- Disubstituted aryl and heteroaryl imines having retinoid-like biological activity
-
Compounds of the formula STR1 wherein the R 1 groups independently are hydrogen, lower alkyl, or two geminal R 1 groups jointly represent an oxo ( O) or a thio ( S) group; R 2 is hydrogen or lower alkyl, or halogen; M is or --N CR 4 -- or --R 4 C N-- where R 4 is hydrogen or lower alkyl; X is C(R 1) 2 ; Y is phenyl optionally substituted with an R 3 group which is lower alkyl or halogen; A is (CH 2) n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR 8, CONR 9 R 10, --CH 2 OH, CH 2OR 11, CH 2 OCOR 11, CHO, CH(OR 12) 2, CHOR 13 O, --COR 7, CR 7 (OR 12) 2, or CR 7 OR 13 O, where R 7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R 8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R 8 is phenyl or lower alkylphenyl, R 9 and R 10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R 11 is lower alkyl, phenyl or lower alkylphenyl, R 12 is lower alkyl, and R 13 is divalent alkyl radical of 2-5 carbons have retinoid-like biological activity.
- -
-
-
- Hypolipidemic and antiatherosclerotic novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs
-
This disclosure described novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.
- -
-
-