- The reaction of prop-2-ynylsulfonium salts and sulfonyl-protected β-amino ketones to epoxide-fused 2-methylenepyrrolidines and S-containing pyrroles
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A novel divergent domino annulation reaction of prop-2-ynylsulfonium salts with sulfonyl-protected β-amino ketones has been developed, affording various epoxide-fused 2-methylenepyrrolidines and S-containing pyrroles in moderate to excellent yields. Prop-2-ynylsulfonium salts act as C2synthons in the reactions providing a promising epoxide-fused skeleton in a single operation with readily accessible starting materials.
- Jia, Tingting,Zeng, Gongruixue,Zhang, Chong,Zeng, Linghui,Zheng, Wenya,Li, Siyao,Wu, Keyi,Shao, Jiaan,Zhang, Jiankang,Zhu, Huajian
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supporting information
p. 2657 - 2660
(2021/03/16)
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- A morpholine group containing pyridine and double protonizing site of the pH of the fluorescent probe, preparation method and application (by machine translation)
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The invention provides a pH fluorescence probe with double-protonation loci of pyridine and morpholine groups and a preparation method and application thereof. The structure of the probe is as shown in formula (I) in the specification. The probe has relatively wide pH response within a pH range of 3.1-5.0, the pKa of the probe is 4.05, in addition, the probe has relatively good water solubleness, optical and chemical stability and relatively good ion selectivity and biological compatibility. Fluorescence microimaging tests show that the probe has relatively good cell permeability and pH response, and has very small cytotoxicity.
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Paragraph 0011; 0027; 0034
(2019/05/28)
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- Monoglycosyl-containing heterocyclic compound for inhibiting hepatitis C viruses and preparation method
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The invention discloses a monoglycosyl-containing heterocyclic compound for inhibiting hepatitis C viruses and a preparation method. The monoglycosyl-containing heterocyclic compound has a chemical structure represented by a formula I shown in the description. The monoglycosyl-containing heterocyclic compound disclosed by the invention can be used for effectively inhibiting protease of the hepatitis C viruses and treating infection of the hepatitis C viruses (HCV).
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Paragraph 0086; 0087
(2019/03/28)
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- PH fluorescent probe by taking pyridine as protonizing site and application thereof
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The invention relates to the technical field of detection, and particularly relates to a novel compound by using 4-(5-phenyl-2-oxazolyl)pyridine as a kernel structure as shown in the general formula (I), as well as a chemical preparation process of the pH fluorescent probe. According to the compound, R1, R2 and R3 are halogen atoms, nitrogen atoms, alkyl, alkoxy or group as shown in the formula IA, wherein Y is a group formed by covalent linkage of methylene, oxygen atom or nitrogen atom with a group as shown in a formula IB (in the formula IB, R5 is hydrogen atom, alkyl or alkoxy, Z1, Z2 and Z3 are null or oxygen atoms, and n, o and p are 0, 1 or 2; R4 represents hydrogen atom, methyl, methoxyl or a group as shown in the formula IB, and m is 0, 1 or 2; R1, R2 and R3 are not halogen atom, hydrogen atom, alkyl or alkoxy at the same time, and X is CH=CH or null, namely a biphenyl structure. The chemical preparation process is applied to fluorescent probe detection on pH value in an aqueous solution, fluorescent probe detection on the pH value in a cell, especially fluorenscense angiography of cells.
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Paragraph 0056; 0060
(2017/08/31)
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- Bromophenol-oxazole compound and its use in drug for treatment on diabetes mellitus type 2
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The invention relates to a chemical total synthesis method of novel bromophenol-oxazole PTP1B and its use in a drug for treatment on diabetes mellitus type 2. The PTP1B inhibitor has a structural formula shown in the description. The compound improves insulin receptor sensibility through inhibiting the activity of protein tyrosine phosphatase 1B and has good treatment effects on insulin resistance-type diabetes mellitus type 2.
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- NOVEL HEPATITIS C VIRUS INHIBITORS
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The invention provides compounds of formula (I): wherein Rings A and A' are independently 5-membered optionally substituted aromatic heterocycles; Q is C(=O)NR1R1' or formula U is C(R4)2, O, S, S(=O)2, C(R4)2C(R4)2, CH2O, OCH2, CH2S, SCH2, CH2S(=O)2, S(=O)CH2 or C=C(Ru )2; X is CH2, CHR12, CR12R12, O, S, S(=O)2 or NRx; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.
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Page/Page column 33; 34
(2013/07/05)
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- CHEMICAL COMPOUNDS
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Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.
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Page/Page column 9-10
(2011/04/14)
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- Synthesis and biological evaluation of imidazol-2-one derivatives as potential antitumor agents
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A new series of aryl substituted imidazol-2-one derivatives structurally related to combretastatin A-4 (CA-4) were synthesized and evaluated for their cytotoxic activities in vitro against various human cancer cell lines including MDR cell line. The cytotoxic effects of compounds 7b and 7i proved to be similar to or greater than that of docetaxel. The highly active compound 7b also exhibited excellent inhibitory activity on tumor growth in vivo.
- Xue, Na,Yang, Xiaochun,Wu, Rui,Chen, Jing,He, Qiaojun,Yang, Bo,Lu, Xiuyang,Hu, Yongzhou
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p. 2550 - 2557
(2008/09/21)
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- Asymmetric hydrogenation of α-primary and secondary amino ketones: Efficient asymmetric syntheses of (-)-arbutamine and (-)-denopamine
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Two ss-receptor agonists (-)-denopamine and (-)-arbutamine were prepared in good yields and enantioselectivities by asymmetric hydrogenation of unprotected amino ketones for the first time by using Rh catalysts bearing electron-donating phosphine ligands. A series of α-primary and secondary amino ketones were synthesized and hydrogenated to produce various 1,2-amino alcohols in good yields and with good enantioselectivies. This Rh electron-donating phosphine-catalyzed asymmetric hyderogenation repI resents one of the most promising and convenient approaches towards the asymmetric synthesis of chiral amino alcohols.
- Shang, Gao,Liu, Duan,Allen, Scott E.,Yang, Qin,Zhang, Xumu
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p. 7780 - 7784
(2008/04/03)
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- THIAZOLE BENZENESULFONAMIDES AS BETA3 AGONISTS FOR TREATMENT OF DIABETES AND OBESITY
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Thiazole substituted benzenesulfonamides are β 3 adrenergic receptor agonists with very little β 1 and β. sub. 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. The compounds are prepared by coupling an aminoalkylphenyl-sulfonamide with an appropriately substituted epoxide. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
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- A Convenient Synthesis of Aminomethyl Ketones (α-Amino Ketones)
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Several N,N-diformylaminomethyl ketones 3 were prepared by treating the respective bromomethylketone 1 with sodium diformylamide in acetonitrile at room temperature.This reaction produced from N-formylaminomethyl ketones 4 when ethanol was used as the solvent.One of the formyl groups of N,N-difomylaminomethyl ketones was selectively removed by using a catalytic amount of sodium or potassium hydroxide in alcohol to the corresponding N-formylaminomethyl ketones 4.The formyl groups of both N,N-diformyl- and N-formylaminomethyl ketones could be easily removed by either5percent hydrochloric acid in ethanol or 6N hydrochloric acid to give the corresponding aminomethyl ketone hydrochlorides 5.These reactions are general and give high yield of the products.
- Yinglin, Han,Hongwen, Hu
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p. 615 - 618
(2007/10/02)
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- Substituted quinolinecarboxylic acids
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Substituted quinolinecarboxylic acids useful in the treatment of arthritis by inhibiting the progressive joint deterioration characteristic of arthritic disease and for inducing immunosuppression are disclosed. Methods of synthesis and use of the novel compounds are also disclosed.
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- A CONVENIENT PREPARATION OF AMINOMETHYL ARYL KETONES AND THEIR DERIVATIVES
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A convenient preparation of N-phenacyl diformamides, N-phenacyl formamides and aminomethyl aryl ketone hydrochlorides from aryl bromomethyl ketones and sodium diformylamide was described.
- Ying-lin, Han,Hong-ven, Hu
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p. 5285 - 5286
(2007/10/02)
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- Antibacterial monic acid derivatives
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A compound of the formula (I) STR1 wherein R is a group STR2 R1 is hydrogen, phenyl, C1-20 alkyl, C2-8 alkenyl or C2-8 alkynyl each of which may optionally be substituted; or C3-7 cycloalkyl, X is a divalent group --Y--C=C--, and Y is oxygen or sulphur, have antibacterial and/or antimycoplasmal activity.
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- Synthesis of 4-oxopyrrolopyrimidine-3-carboxylic acid derivatives as potential antimicrobial agents
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A route for the synthesis of various derivatives of 4-oxopyrrolopyrimidine-3-carboxylic acid from 2-amino-3-cyano-4,5-dimethylpyrrole and 2-amino-3-cyano-4-arylpyrroles is described.
- Bayomi, Said M.,Al-Obaid, Abdul Rahman M.,Jado, Ahmad I.,Loutfy, Essam A.
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p. 814 - 816
(2007/10/02)
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- SYNTHESIS OF ARYLAZOLES AND THEIR LUMINESCENT PROPERTIES
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The luminescent spectral properties of aryl derivatives of indole, oxazole, thiazole, benzoxazole, benzothiazole, and oxadiazole have been studied.
- Andreeshchev, E. A.,Viktorova, V. S.,Kilin, S. F.,Kovyrzina, K. A.,Kosyakina, L. N.,at al.
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p. 1262 - 1266
(2007/10/02)
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- 5-(4-Bromophenyl)oxazole
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The compound 5-(4-bromophenyl)oxazole is useful as an antifungal agent.
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