90794-32-4Relevant academic research and scientific papers
Synthesis of carbonylated heteroaromatic compounds: Via visible-light-driven intramolecular decarboxylative cyclization of o -alkynylated carboxylic acids
Gao, Fei,Wang, Jiu-Tao,Liu, Lin-Lin,Ma, Na,Yang, Chao,Gao, Yuan,Xia, Wujiong
supporting information, p. 8533 - 8536 (2017/08/04)
An efficient strategy for the easy access to carbonylated heteroaromatic compounds has been developed via a visible-light-promoted intramolecular decarboxylative cyclization reaction of o-alkynylated carboxylic acids. This method is characterized by its b
Enantioselective Intramolecular C?H Insertion of Donor and Donor/Donor Carbenes by a Nondiazo Approach
Zhu, Dong,Ma, Jun,Luo, Kui,Fu, Hongguang,Zhang, Li,Zhu, Shifa
supporting information, p. 8452 - 8456 (2016/07/19)
The first enantioselective intramolecular C?H insertion and cyclopropanation reactions of donor- and donor/donor-carbenes by a nondiazo approach are reported. The reactions were conducted in a one-pot manner without slow addition and provided the desired
PYRAZOLO[3,4-D]PYRIMIDIN-4(5H)-ONE DERIVATIVES AS PDE9 INHIBITORS
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Page/Page column 24; 26, (2014/02/16)
A compound of the general formula (I) wherein R1 is selected from the group consisting of phenyl unsubstituted or substituted with 1 to 3 substituents selected from F, Cl, Br, I, CN, -O-C1-C3-alkyl, fluorinated -O-C1-C3-alkyl, -(CH2)mOH and 5-membered heterocyclic group with 1 or 2 heteroatoms selected from N, O and S; and 6- or 10-membered heteroaryl with 1 to 3 heteroatoms selected from O, N and S; R2 and R3 independently of each other represent H atom or straight or branched C1-C3 alkyl; R4 is selected from the group consisting of 4- to 6- membered cycloalkyl, wherein one of carbon atoms can be replaced by O atom, and which is unsubstituted or substituted with one or two halogen atoms,and straight or branched C1-C4 alkyl; Q represents a bond or C1-C3-alkylene, which can be optionally substituted by one to three C1-C3-alkyls; X is selected from the group consisting of O, NR5, and S(O)p; R5 represents H atom or C1-C3alkyl; m is 1, 2 or 3; p is 0, 1 or 2; and salts thereof, for use as a medicament, in particular for treating cognitive function disorders and neurodegenerative diseases.
PRMT5 INHIBITORS AND USES THEREOF
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Paragraph 00240, (2014/07/08)
Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.
Synthesis and biological evaluation of new quinoxaline derivatives of ICF01012 as melanoma-targeting probes
El Aissi, Radhia,Liu, Jianrong,Besse, Sophie,Canitrot, Damien,Chavignon, Olivier,Chezal, Jean-Michel,Miot-Noirault, Elisabeth,Moreau, Emmanuel
supporting information, p. 468 - 473 (2014/06/09)
The aim of this study was the synthesis and pharmacokinetic selection of a best melanin-targeting ligand for addressing anticancer agents to pigmented melanoma. Seven quinoxaline carboxamide derivatives were synthesized and radiolabeled with iodine-125. Biodistribution studies of compounds [ 125I]1a-g performed in melanoma-bearing mice tumor showed significant tumor uptake (range 2.43-5.68%ID/g) within 1 h after i.v. injection. Fast clearance of the radioactivity from the nontarget organs mainly via the urinary system gave high tumor-to-blood and tumor-to-muscle ratios. Given its favorable clearance and high tumor-melanoma uptake at 72 h, amide 1d was the most promising melanoma-targeting ligand in this series. Compound 1d will be used as building block for the design of new melanoma-selective drug delivery systems.
Palladium-catalyzed, microwave-assisted synthesis of 3,4-dihydro-3-oxo-2 H -1,4-benzoxazines: An improved catalytic system and multicomponent process
Feng, Gaofeng,Wang, Shengnan,Li, Weiting,Chen, Fengjiang,Qi, Chenze
, p. 2711 - 2718 (2013/10/21)
An improved palladium-catalyzed system is established for the synthesis of 3,4-dihydro-3-oxo-2H-1,4-benzoxazines from less reactive ethyl 2-(2-chlorophenoxy)alkanoates and aryl amines under controlled microwave heating, employing 2-dicyclohexylphosphino-2′,4′,6′- triisopropylbiphenyl (XPhos) as the ligand. Moreover, a high-yielding, three-component reaction protocol is disclosed for the efficient one-pot synthesis of 3,4-dihydro-3-oxo-2H-1,4-benzoxazines from 2-halophenols, ethyl 2-bromoalkanoates, and aryl amines. Microwave heating at high temperature is necessary to achieve high yields with 2-chlorophenol. A wide range of substrates is tolerated affording the desired products in good to excellent yields.
DBU-mediated regioselective intramolecular cyclization/dehydration of ortho diketo phenoxyethers: A synthesis of 2,3-substituted γ-benzopyranones
Bensulong, Sofia,Boonsombat, Jutatip,Ruchirawat, Somsak
, p. 9335 - 9348 (2013/10/01)
The regioselective cyclization/dehydration sequence of ortho diketo phenoxyethers induced by DBU has been explored. The results demonstrated a high degree of selectivity with preference for 6-exo-trig cyclization leading to the formation of γ-benzopyranone derivatives in good yield.
A Pd-catalyzed cascade protocol towards 2-alkyl-4-aryl-4H-benz[1,4]oxazin- 3-ones from aryl amines and 2-(2-halophenoxy)alkanoates
Feng, Gaofeng,Yin, Fangling,Chen, Fengjiang,Song, Qingbao,Qi, Chenze
supporting information; experimental part, p. 601 - 606 (2012/03/27)
A cascade process, consisting of Pd-catalyzed intermolecular amination and subsequent thermal intramolecular amidation, has been established for efficient one-pot synthesis of 4H-benz[1,4]oxazin-3-ones from anilines and 2-(2-halophenoxy)alkanoates. Use of
A 1,4-diphenyl-1,2,3-triazole-based β-turn mimic constructed by click chemistry
Wu, Chun-Fang,Zhao, Xin,Lan, Wen-Xian,Cao, Chunyang,Liu, Jin-Tao,Jiang, Xi-Kui,Li, Zhan-Ting
experimental part, p. 4261 - 4270 (2012/06/18)
A series of 1,4-diphenyl-1,2,3-triazole-incorporated amide derivatives have been designed and prepared. X-ray crystallographic and (1D and 2D) 1H NMR studies reveal that these compounds fold into stable U-shaped conformations driven by three-center intramolecular C-H???O hydrogen-bonding formed between the triazole C-5 H atom and the two ether O atoms. Such folded structures make this 1,4-diphenyl-1,2,3-triazole skeleton a good candidate to be used as β-turn mimic. To prove this, the formation of a β-hairpin structure induced by this β-turn motif has been further demonstrated.
Phase-transfer-catalyzed intramolecular cyclization of ortho-alkynyl phenyl ether derivatives for synthesis of 2,3-disubstituted benzo[b]furans
Hu, Jie,Wu, Lu-Yong,Wang, Xiang-Chuan,Hu, Yuan-Yuan,Niu, Yan-Ning,Liu, Xue-Yuan,Yang, Shangdong,Lianga, Yong-Min
supporting information; experimental part, p. 351 - 356 (2010/04/28)
A variety of substituted benzo[b]furans are readily prepared in good to excellent yields under the mild reaction conditions from o-(1-alkyn-ylphenoxy)- 1-phenylethanone under phase-transfer catalysis (PTC). This methodology accommodates simple experimenta
