- MANUFACTURING METHOD OF AROMATIC IODINE COMPOUND USING DISULFIDE AS CATALYST
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To manufacture an aromatic iodine compound under a mild condition at low cost and high yield.SOLUTION: There is provided a manufacturing method of an aromatic iodine compound by reacting an aromatic compound and an iodination agent in a presence of a cata
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Paragraph 0022
(2020/04/04)
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- Fused tetracyclic compounds and application thereof in medicines
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The invention relates to fused tetracyclic compounds and an application thereof in medicines, and in particular, relates to the application of the fused tetracyclic compounds as medicines for treatingand/or preventing hepatitis B. Specifically, the invention relates to the compounds represented by a general formula (I) or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, wherein the variables are defined in the specification. The invention further relates to the application of the compounds represented by the general formula (I) or the stereoisomers, the tautomers, the nitric oxides, the solvates, the metabolites, the pharmaceutically acceptable salts or the prodrugs thereof as medicines, and in particular, relates tothe application of the compounds as the medicines for treating and/or preventing hepatitis B.
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Paragraph 0344; 0346-0348
(2020/04/17)
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- Silver(I)-catalyzed iodination of arenes: Tuning the lewis acidity of N-iodosuccinimide activation
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A mild and rapid method for the iodination of arenes that utilizes silver(I) triflimide as a catalyst for activation of N-iodosuccinimide has been developed. The transformation was found to be general for a wide range of anisole, aniline, acetanilide, and phenol derivatives and allowed the late-stage iodination of biologically active compounds such as PIMBA, a SPECT imaging agent of breast cancer, and (a?)-IBZM, a dopamine D2 receptor antagonist. The method was also modified for the radioiodination of arenes using a one-pot procedure involving the in situ generation of [125I]-N-iodosuccinimide followed by the silver(I)-catalyzed iodination.
- Racys, Daugirdas T.,Sharif, Salaheddin A. I.,Pimlott, Sally L.,Sutherland, Andrew
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p. 772 - 780
(2016/02/18)
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- Highly Regioselective Iodination of Arenes via Iron(III)-Catalyzed Activation of N-Iodosuccinimide
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An iron(III)-catalyzed method for the rapid and highly regioselective iodination of arenes has been developed. Use of the powerful Lewis acid, iron(III) triflimide, generated in situ from iron(III) chloride and a readily available triflimide-based ionic liquid allowed activation of N-iodosuccinimide (NIS) and efficient iodination under mild conditions of a wide range of substrates including biologically active compounds and molecular imaging agents.
- Racys, Daugirdas T.,Warrilow, Catherine E.,Pimlott, Sally L.,Sutherland, Andrew
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supporting information
p. 4782 - 4785
(2015/10/12)
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- Mild arming and derivatization of natural products via an In(OTf) 3-catalyzed arene iodination
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Figure presented Iodination of arene-containing natural products employing N-iodosuccinimide catalyzed by In(OTf)3 at ambient temperature is reported as a versatile and mild method for natural product derivatization amenable to small scale. This process facilitates natural product derivatization of arene moieties for SAR studies, homo- and heterodimerization of natural products, and also conjugation with reporters such as biotin via subsequent metal-mediated coupling reactions.
- Zhou, Cong-Ying,Li, Jing,Peddibhotla, Satyamaheshwar,Romo, Daniel
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supporting information; experimental part
p. 2104 - 2107
(2010/09/15)
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- Copper-catalyzed arene C-H bond cross-coupling
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A highly regioselective, one-pot sequential iodination-copper-catalyzed cross-coupling of arene C-H bonds has been developed affording an efficient method for biaryl synthesis.
- Do, Hien-Quang,Daugulis, Olafs
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supporting information; experimental part
p. 6433 - 6435
(2010/03/04)
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- Synthesis of 5-iodobenzofurans and 6-iodobenzopyrans via direct iodination with mercury(II) oxide-iodine reagent
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A tin(IV) chloride assisted iodo-cyclization of 2-allylphenol gave 2-iodomethyl-2,3-dihydrobenzofuran. A similar cyclization of 2-crotylphenol gave 3-iodo-2-methyl-3,4-dihydro-2H-benzopyran, exclusively. By iodination with mercury(II) oxide-iodine reagent in dichloromethane, 2,3-dihydrobenzofurans or 3,4-dihydro-2H-benzopyrans including the above benzocyclic ethers were easily converted to the corresponding 5- or 6-iodo derivatives, regioselectively, in good yield.
- Orito, Kazuhiko,Hatakeyama, Takahiro,Takeo, Mitsuhiro,Suginome, Hiroshi,Tokuda, Masao
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- Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2
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The preparations of thienotriazolodiazepines bearing a substituted ethynyl group at the 2-position, and the corresponding cis-olefins and fully saturated analogues are described. The compounds were evaluated as potential antagonists of platelet-activating
- Walser,Flynn,Mason,Crowley,Maresca,O'Donnell
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p. 1440 - 1446
(2007/10/02)
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