- Enantioselective decarboxylative Mannich reaction of β-keto acids withC-alkynylN-BocN,O-acetals: access to chiral β-keto propargylamines
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The chiral keto-substituted propargylamines are an essential class of multifunctional compounds in the field of organic and pharmaceutical synthesis and have attracted considerable attention, but the related synthetic approaches remain limited. Therefore, a concise and efficient method for the enantioselective synthesis of β-keto propargylaminesviachiral phosphoric acid-catalyzed asymmetric Mannich reaction between β-keto acids andC-alkynylN-BocN,O-acetals as easily availableC-alkynyl imine precursors has been demonstrated here, affording a broad scope of β-ketoN-Boc-propargylamines in high yields (up to 97%) with generally high enantioselectivities (up to 97?:?3 er).
- Chen, Li-Jun,Li, Wei,Shen, Bao-Chun,Sun, Zhong-Wen,Xie, Hui-Ding,Zhang, Cong-Cong
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supporting information
p. 8607 - 8612
(2021/10/20)
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- Picolinamide compound containing triazole or quinolinone structure and application of picolinamide compound
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The invention provides a picolinamide compound containing a triazole or quinolinone structure and application of the picolinamide compound. According to a technical scheme in the invention, extensiveresearch is conducted on the picolinamide compound, and
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Paragraph 0226; 0243-0244
(2020/01/12)
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- Discovery of novel pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety as potential antitumor inhibitor
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A series of pyrrolo[2,3-b]pyridine derivatives bearing 4-oxoquinoline moiety were designed, synthesized and evaluated for the anti-proliferative on three cancer cell lines (A549, HepG2 and MCF-7) in vitro. Most of the compounds showed moderate to high potency. Some excellent compounds were tested for the inhibitory activity of c-Met kinase. Compound 34 (c-Met IC50 = 17 nM) was investigated the selectivity against Flt-3, c-Kit, VEGFR-2, ALK, PDGFR-β and RON. Structure-activity relationship studies indicated that hydrogen, fluorine atom, and mono-electron-withdrawing groups (mono-EWGs, such as R2 = F) on R, R1 and R2, respectively, were beneficial for the anti-proliferative activities of the target compounds. Besides, we have took further study on the combined mode between compound 34 and c-Met kinase through molecular docking.
- Chen, Ting,Duan, Yongli,Huang, Shunmin,Liu, Huimin,Tang, Qidong,Xiong, Hehua,Zhang, Jianqing,Zheng, Pengwu
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- Amide compound and application thereof as TGR5 agonist
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Belonging to the technical field of medicine, the invention in particular relates to an amide TGR5 agonist compound shown as formula (I), its pharmaceutically acceptable salts, esters, stereoisomers, solvent compounds or prodrugs, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, X, Y, Z, and ring A are defined as the specification. The invention also relates to a preparation method of the compounds, pharmaceutical preparations, pharmaceutical compositions, and application of the compounds in preparation of drugs for treatment and/or prevention of TGR5 activity regulation related diseases. (formula (I)).
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Paragraph 0214-0216
(2017/04/20)
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- Geminal Dichlorination of Phenyliodonium Ylides of β-Dicarbonyl Compounds through Double Ligand Transfer from (Dichloroiodo)benzene
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Pre-formed phenyliodonium ylides of cyclic and acyclic β-diketones, β-keto esters and β-diesters were reacted with (dichloroiodo)benzene, resulting in transfer of both chloride ligands onto the ylidic carbon. These two hypervalent iodine(III) compounds exhibit high reactivity towards each other under mild reaction conditions and typically afford the gem-dichloride products in good yield. Upon comparison of these chlorination reactions with those of the analogous diazocarbonyl compounds, reactions of iodonium ylides were unilaterally faster, and often gave the products in higher yield.
- Tao, Jason,Tuck, Tina N.,Murphy, Graham K.
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supporting information
p. 772 - 782
(2016/03/01)
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- Formation of substituted 1-naphthols and related products via dimerization of alkyl 3-(o-halo(het)aryl)-oxopropanoates based on a CuI-catalyzed domino C-arylation/condensation/aromatization process
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Substrates bearing both a β-ketoester moiety and a (het)aryl halide structure element were dimerized to 1-naphthols and related products in the presence of catalytic amounts of CuI in isopropanol. The reaction starts with an intermolecular C-arylation, which is followed by an intramolecular condensation. The final aromatization delivers the highly substituted products with yields up to 81%.
- Weischedel, Heike,Sudheendran, Kavitha,Mikhael, Alevtina,Conrad, Jürgen,Frey, Wolfgang,Beifuss, Uwe
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p. 3454 - 3467
(2016/06/06)
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- Transition metal-free one-pot synthesis of 2-substituted 3-carboxy-4-quinolone and chromone derivatives
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A novel one-pot synthesis of the 2-substituted 3-carboxy-4-quinolone/ chromone derivatives from readily available 3-oxo-3-arylpropanoates and amides/acyl chlorides is reported, without any transition metal aid. The Royal Society of Chemistry 2013.
- Lin, Jian-Ping,Long, Ya-Qiu
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supporting information
p. 5313 - 5315
(2013/06/27)
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- HOTf mediated cascade reactions of 1-arenoylcyclopropanecarboxylic acids with arenes
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The cascade reactions of 1-arenoylcyclopropanecarboxylic acids with arenes proceed smoothly in freshly distilled HOTf to give the corresponding tetrahydro-5H-benzo[c]fluorene derivatives in good yields along with high stereoselectivities under mild conditions. The Royal Society of Chemistry.
- Chen, Gen-Qiang,Tang, Xiang-Ying,Shi, Min
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supporting information; scheme or table
p. 2340 - 2342
(2012/04/18)
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- Synthesis and biological activity of new (E)-α-(Methoxyimino) benzeneacetate derivatives containing a substituted pyrazole ring
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Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin analogues with high activity, a series of new strobilurin derivatives containing a substituted pyrazole in the side chain were synthesized and their biological activities were tested. The compounds were identified by 1H nuclear magnetic resonance, infrared, and elemental analysis. The test results indicated that the compounds exhibited strong fungicidal activities against Pyricularia oryzae, Phytophthora infestans, Pseudoperonospora cubenssi, and Erysiphe graminis. The relationship between structure and biological activity is discussed in terms of the effects of the substituents on the pyrazole ring. The present work demonstrates that strobilurin analogues with a 3-(substituted phenyl)-1 H-pyrazol-5-oxy side chain can be used as possible lead compounds for the development of potential agrochemicals.
- Li, Miao,Liu, Chang-Ling,Yang, J.I.-Chun,Zhang, Jin-B.O.,Li, Zhi-Nian,Zhang, Hong,Li, Zheng-Ming
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experimental part
p. 2664 - 2667
(2011/08/05)
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- Highly enantioselective synthesis of β-amino acid derivatives by the lewis base catalyzed hydrosilylation of β-enamino esters
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A study was conducted to demonstrate highly enantioselective synthesis of β-amino acid derivatives by the Lewis base catalyzed hydrosilylation of βenamino esters. It was found that these catalyst and its analogue displayed excellent activities and enantioselectivities in promoting hydrosilylation of N-aryl β-enamino esters. N-picolinoylpyrrolidine derivatives and N-picolioylephedrine were also evaluated in hydrosilylation of (Z)-methyl 3-phenyl-3-(phenylamino)acrylate. The generality of the Lewis base organocatalyzed hydrosilylation of various β-enamino esters were examined under the optimized conditions. It was observed that the catalytic system exhibited a high sensitivity to the N-substituents, while all the N-aryl β-enamino esters underwent the hydrosilylation smoothly to give corresponding β-amino esters.
- Zheng, Hong-Jie,Chen, Wen-Bing,Wu, Zhi-Jun,Deng, Jin-Gen,Lin, Wen-Qing,Yuan, Wei-Cheng,Zhang, Xiao-Mei
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supporting information; experimental part
p. 9864 - 9867
(2009/10/02)
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- FUSED PYRAZOLE AS p38 MAP KINASE INHIBITORS
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Fused pyrazoles effective as p38 MAP kinase inhibitors, methods of making the compounds, and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
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Page/Page column 40
(2008/06/13)
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- Heteroaryl-fused pyrazolo derivatives and methods for using the same
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Compounds of the formula I: where A, B, X, Y, Z, k, R1, R2 and R3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using t
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Page/Page column 42
(2010/02/13)
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