- Synthesis method of 2-halogen-5-iodobenzoic acid
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The invention discloses a synthesis method of 2-halogen-5-iodobenzoic acid. The synthesis method comprises steps as follows: o-halogen benzoic acids are subjected to one-step iodo treatment in an iodio reagent, and 2-halogen-5-iodobenzoic acid is obtained. Aftertreatment comprises steps as follows: a reaction liquid is poured into a cold reductive water solution and quenched, a solvent is evaporated to dryness, recrystallization and filtration are performed, and a product can be obtained. The method is short in reaction route, simple to operate, environmentally friendly, safer and more economical and has broad application prospects.
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Paragraph 0043-0047
(2019/09/17)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- Novel HIV-1 integrase inhibitors derived from quinolone antibiotics
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The viral enzyme integrase is essential for the replication of human immunodeficiency virus type 1 (HIV-1) and represents a remaining target for antiretroviral drugs. Here, we describe the modification of a quinolone antibiotic to produce the novel integr
- Sato, Motohide,Motomura, Takahisa,Aramaki, Hisateru,Matsuda, Takashi,Yamashita, Masaki,Ito, Yoshiharu,Kawakami, Hiroshi,Matsuzaki, Yuji,Watanabe, Wataru,Yamataka, Kazunobu,Ikeda, Satoru,Kodama, Eiichi,Matsuoka, Masao,Shinkai, Hisashi
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p. 1506 - 1508
(2007/10/03)
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- 4-hydroxycinnoline-3-carboxyamides as antiviral agents
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Certain novel 4-hydroxycinnoline-3-carboxyamides. The compounds are particularly effective in the treatment or prevention of viral infections, particularly infections caused by herpes viruses including herpes simplex virus types 1 and 2, human herpes viru
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- 4-oxo-1,4-dihydro-3-cinnolinecarboxamides as antiviral agents
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This invention provides compounds of formula I; which are useful as antiviral agents.
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- 4-oxo-1,4-dihydro-3-quinolinecarboxamides as antiviral agents
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The present invention provides a compound of formula I Wherein R1is C1-7alkyl, optionally substituted by hydroxy or NR4R5; R2is C1-7alkyl substituted by hydroxy or NR4R5; R3is H, F or C1-7alkoxy; R4and R5together with N are a 5- or 6-membered heterocyclic moiety having 1-3 heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur in which sulfur may be substituted by one (1) or two (2) oxygen atoms; and pharmaceutically acceptable salts thereof Compounds of formula I of the present invention are useful as antiviral agents.
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- Quinolinecarboxamides as antiviral agents
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The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
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- From peptide to non-peptide. 3. Atropisomerie GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus
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The benzodiazepinedione class of non-peptidal GPIIbIIIa antagonists has been modified to allow the isolation of noninterconverting rotational isomers, or atropisomers, with the aim of examining their structure-activity relationships as compared to active
- Blackburn, Brent K.,Lee, Arthur,Baier, Mark,Kohl, Benjamin,Olivero, Alan G.,Matamoros, Regina,Robarge, Kirk D.,McDowell, Robert S.
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p. 717 - 729
(2007/10/03)
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- Fluorine as an ortho-directing group in aromatic metalation: Generality of the reaction and the high position of fluorine in the Dir-Met potency scale
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Many para-substituted fluorobenzenes can be lithiated ortho to fluorine in moderate to good yields, often with one of the dialkylamide bases, lithium diisopropylamide (LDA) or lithium 2,2,6,6-tetramethylpiperidide (LiTMP). Intramolecular competition experiments reveal that fluorine is one of the most potent Dir-Met activating groups under these conditions.
- Bridges,Lee,Maduakor,Schwartz
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p. 7495 - 7498
(2007/10/02)
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- Pyrido[2,3-d]pyrimidine derivatives
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Derivatives of N-[2-(5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-6-yl)-alkyl]benzoyl-L-glutamic acid are antineoplastic agents. A typical embodiment is N-(2-fluoro-4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido-[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-gluta
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