- Quinoxaline compound, preparation method and application of quinoxaline compound in medicine
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The invention provides a quinoxaline compound, a preparation method and application of the quinoxaline compound in medicine, and particularly relates to a quinoxaline compound with PAR4 antagonistic activity, a preparation method of the quinoxaline compound, a pharmaceutical composition containing the quinoxaline compound and application of the quinoxaline compound. Specifically, the invention provides a compound shown as a general formula I and/or II or a tautomer or pharmaceutically acceptable salt thereof, a preparation method of the compound, and application of the compound or the tautomer or the pharmaceutically acceptable salt in medicines for preventing and/or treating thromboembolic diseases.
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Paragraph 0177-0180
(2021/07/24)
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- Benzotriazine compound with PAR4 antagonistic activity and application thereof
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The invention discloses a benzotriazine compound with PAR4 antagonistic activity and application thereof. The present invention relates to a compound of formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt, ester, solvate or prodrug t
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Paragraph 0059; 0061-0062
(2020/08/02)
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- BICYCLIC HETEROARYL SUBSTITUTED COMPOUNDS
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Disclosed are compounds of Formula (I) to (VIII): (I) (II) (III) (IV) (V) (VI) (VII) (VIII); or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a bicyclic heteroaryl group substituted with zero to 3 R3a; and R1, R2, R3a, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
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Page/Page column 454
(2018/03/25)
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- Inexpensive NaX (X = I, Br, Cl) as a halogen donor in the practical Ag/Cu-mediated decarboxylative halogenation of aryl carboxylic acids under aerobic conditions
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Versatile and practical Ag/Cu-mediated decarboxylative halogenation between readily available aryl carboxylic acids and abundant NaX (X = I, Br, Cl) has been achieved under aerobic conditions in moderate to good yields. The halodecarboxylation is shown to be an effective strategy for S-containing heteroaromatic carboxylic acid and benzoic acids with nitro, chloro and methoxyl substituents at the ortho position. A gram-scale reaction and a three-step procedure to synthesize iniparib have been performed to evaluate the practicality of this protocol. A preliminary mechanistic investigation indicates that Cu plays a vital role and a radical pathway is involved in the transformation.
- Fu, Zhengjiang,Jiang, Ligao,Zuo, Qianming,Li, Zhaojie,Liu, Yanzhu,Wei, Zhenhong,Cai, Hu
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supporting information
p. 5416 - 5421
(2018/08/12)
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- Synthetic method of aryl halide taking aryl carboxylic acid as raw material
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A synthetic method of an aryl halide taking aryl carboxylic acid as a raw material is characterized in that a corresponding aryl halide is formed by carrying out substitution reaction on an aryl carboxylic acid compound and haloid salt MX in an organic solvent under the condition that oxygen, a silver catalyst, a copper additive and a bidentate nitrogen ligand exist, wherein M in MX represents alkali metal or alkaline earth metal, and X represents F, Cl, Br or I. Compared with a conventional aryl halide synthetic method, the synthetic method disclosed by the invention has the obvious advantages that reaction raw materials (comprising aryl carboxylic acid and MX) are cheap and easy to obtain, the using amount of a metal catalyst is small, pollution to the environment when the oxygen is used as an oxidant is the smallest, good tolerance to various functional groups on an aromatic ring is obtained, the yield is high, and the like. The synthetic method disclosed by the invention can be widely applied to synthesis in the fields of medicine, materials, natural products and the like in industry and academia.
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Paragraph 0133
(2018/01/03)
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- Production method of 3-ethoxy-4-nitrophenol
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The invention discloses a production method of 3-ethoxy-4-nitrophenol. The low-price m-dichlorobenzene is used instead of the high-price resorcinol as the raw material, and the methoxy is converted into the hydroxy; and a simple alkaline process is used instead of the conventional hydrogen bromide/acetic acid system to prepare the 3-ethoxy-4-nitrophenol. By using low-price m-dichlorobenzene instead of the high-price resorcinol as the raw material to prepare the 3-ethoxy-4-nitrophenol, the method has the advantages of simple synthesis steps, low pollution, environment friendliness, high product quality, high yield, low production cost and normal-pressure operation, and can implement industrial production.
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Paragraph 0035
(2017/05/26)
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- Decarboxylative Halogenation and Cyanation of Electron-Deficient Aryl Carboxylic Acids via Cu Mediator as Well as Electron-Rich Ones through Pd Catalyst under Aerobic Conditions
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Simple strategies for decarboxylative functionalizations of electron-deficient benzoic acids via using Cu(I) as promoter and electron-rich ones by employing Pd(II) as catalyst under aerobic conditions have been established, which lead to smooth synthesis of aryl halides (-I, Br, and Cl) through the decarboxylative functionalization of benzoic acids with readily available halogen sources CuX (X = I, Br, Cl), and easy preparation of benzonitriles from decarboxylative cyanation of aryl carboxylic acids with nontoxic and low-cost K4Fe(CN)6 under an oxygen atmosphere for the first time.
- Fu, Zhengjiang,Li, Zhaojie,Song, Yuanyuan,Yang, Ruchun,Liu, Yanzhu,Cai, Hu
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p. 2794 - 2803
(2016/04/26)
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- Silver-catalyzed decarboxylative halogenation of carboxylic acids
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Decarboxylative halogenation of carboxylic acids catalyzed by silver carbonate is reported. ortho-Nitrobenzoic acids react with copper(II) chloride or bromide in DMF/DMSO at 130-140 °C leading to the corresponding aryl halides in moderate to good yields.
- Luo, Yong,Pan, Xiaolin,Wu, Jie
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supporting information; experimental part
p. 6646 - 6648
(2011/02/21)
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- KINASE INHIBITORS AND METHODS OF USE
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The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.
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Page/Page column 81-82
(2010/04/03)
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- Nitration of some aromatic compounds by sodium nitrate in the presence of benzyltriphenylphosphonium peroxodisulfate
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A simple, mild, and regioselective method for the nitration of some aromatic compounds using sodium nitrate in the presence of benzyltriphenylphosphonium peroxodisulfate in acetonitrile as solvent is reported. Mild reaction conditions and good to excellent yields of the products are the noteworthy advantages of the method. Copyright Taylor & Francis Group, LLC.
- Tajik, Hassan,Zolfigol, Mohammad Ali,Albadi, Jalal,Eslami, Ramin
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p. 2771 - 2776
(2008/02/12)
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- Compounds having cGMP-PDE inhibitory effect
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Novel fused tetracyclic heterocyclic compounds having a potent and highly selective effect of inhibiting cyclic GMP phosphodiesterase (cGMP-PDE) and a high safety; a process for producing the same; drugs characterized by containing at least one of these compounds as the active ingredient, in particular, preventives and/or remedies for pulmonary hypertension, ischemic heart diseases, erectile insufficiency, female sexual dysfunction or diseases against which cGMP-PDE inhibitory effects are efficacious and intermediates useful in producing the above compounds.
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- Synthesis of functionalized indole- and benzo-fused heterocyclic derivatives through anionic benzyne cyclization
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The development of a new method for the regioselective synthesis of functionalized indoles and six-membered benzo-fused N-, O-, and S-heterocycles is reported. The key step involves the generation of a benzyne-tethered vinyl or aryllithium compound that undergoes a subsequent intramolecular anionic cyclization. Reaction of the organolithium intermediates with selected electrophiles allows the preparation of a wide variety of indole, tetrahydrocarbazole, dihydrofenantridine, dibenzopyran, and dibenzothiopyran derivatives. Finally, the application of this strategy to the appropriate starting materials allows the preparation of some tryptamine and serotonin analogues.
- Barluenga, Jose,Fananas, Francisco J.,Sanz, Roberto,Fernandez, Yolanda
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p. 2034 - 2046
(2007/10/03)
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- Transition metal complexes in organic synthesis. Part 46: Synthesis of 5-arylmethyl-substituted tricarbonyl(1-4-η-cyclohexa-1,3-diene)iron complexes
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The reaction of tricarbonyl(η5-cyclohexadienylium) iron tetrafluoroborate 3 with the methyl arylacetate 6, the dimethyl arylmalonate 12, and the di-tert-butyl arylmalonate 14 provides regio- and stereoselectively the tricarbonyliron-complexed 5
- Knoelker, Hans-Joachim,Graf, Michael,Mangei, Ulrike
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experimental part
p. 530 - 535
(2011/10/12)
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- Indoloquinone compounds
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Indoloquinone compounds useful as cytostatic agents have formula (I), where R2 and R3 are in each case, hydrogen, halogen, an alkyl group (which may be substituted), an alkoxy group or an aryloxy group, an alkylthio group or an arylt
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