- Method for preparing 1-benzyl-3-hydroxy-1H-3-indazole sodium salt
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The invention relates to a method for preparing 1-benzyl-3-hydroxy-1H-3-indazole sodium salt. The method is characterized in that o-aminobenzoic acid, concentrated hydrochloric acid, a NaNO2 solution and solid Na2SO3 are taken as starting raw materials, a proper amount of a NaOH solution and a proper amount of benzyl chloride are added, and 1-benzyl-3-hydroxy-1H-3-indazole sodium salt is obtained through multi-step reaction filtering dehydration. The method is easily accessible in raw material, mild in reaction condition, low in cost and suitable for factory large-scale production.
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- Synthesis of Indazolones via Friedel-Crafts Cyclization of Blocked (Masked) N-Isocyanates
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Nitrogen-substituted isocyanates (N-isocyanates) are rare amphoteric reagents with high, but underdeveloped synthetic potential. Herein, we study the formation of indazolones by Friedel-Crafts cyclization of N-isocyanates using blocked (masked) N-isocyanate precursors: the effect of the masking group and the reaction scope have been delineated. Substrate synthesis has also been improved using a reported copper-catalyzed coupling of arylbismuth(V) reagents that is compatible with the hemilabile OPh blocking group.
- Elkaeed, Eslam B.,An, Jing,Beauchemin, André M.
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p. 9890 - 9897
(2017/09/23)
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- ORGANIC DICARBOXYLIC ACIDS, SALTS AND PREPARATION METHOD THEREOF
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Organic dicarboxylic acid compounds, salts and preparation methods thereof. The said compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as formula (1).
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Page/Page column 2
(2012/09/11)
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- Polyfluoroalkylation and alkenylation of 1-benzyl-1H-indazol-3-ol
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The polyfluoroalkylation and alkenylation of 1-benzyl-1H-indazol-3-ol by halopolyfluoroalkanes and fluorinated olefins has been studied. It was shown that only reactions proceeding with the participation of difluorocarbene lead to a mixture of N- and O-alkylation products. In all other cases, interaction with halopolyfluoroethanes and polyfluoroalkenes forms O-polyfluoroalkyl and alkenyl derivatives of indazolol.
- Sokolenko,Yagupolskii
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experimental part
p. 1335 - 1343
(2011/10/30)
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- Synthesis and biological evaluations of novel bendazac lysine analogues as potent anticataract agents
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Novel bendazac analogues and their salts have been designed and prepared. The resulting compounds (13c-d, 15c, 17c) showed very good aqueous solubility (>100 mg/mL). An in vitro assay showed that most of the resulting compounds had potent protective activ
- Shen, Hong,Gou, Shaohua,Shen, Jianping,Zhu, Yanqin,Zhang, Yindi,Chen, Xuetai
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scheme or table
p. 2115 - 2118
(2010/06/19)
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- Copper-catalyzed mild and efficient entry to 1-substituted indazolones
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A variety of 1-alkyl- and aryl-substituted indazolones were synthesized easily starting from commercially available 2-halobenzoic acids and hydrazines via the copper-catalyzed intramolecular C-N bond formation of 2-halobenzohydrazides under mild conditions.
- Tanimori, Shinji,Ozaki, Yuka,Iesaki, Yasukazu,Kirihata, Mitsunori
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body text
p. 1973 - 1976
(2009/05/27)
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- INDAZOLE DERIVATIVES THAT ARE ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE
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Compounds of formula (I) are novel indazoles useful for increasing cGMP levels in a mammal.
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Page/Page column 28
(2010/02/07)
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- An improved synthesis of YC-1
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A concise synthesis of YC-1 has been achieved in ten-fold enhanced yield over the previously reported method. This new, flexible strategy should readily allow the automated parallel synthesis of analogues.
- Gordon, David W.
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p. 1065 - 1066
(2007/10/03)
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- Selective synthesis of 2-substituted indazolin-3-ones without N-1 protection
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N-2-Alkylation of indazolin-3-ones was performed in neutral conditions. This method represents a direct and efficient entry to a class of compounds having interesting biological activities, avoiding the generally required N-1 protection.
- Arán, Vicente J.,Díez-Barra, Enrique,De La Hoz, Antonio,Sánchez-Verdú, Prado
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p. 129 - 136
(2007/10/03)
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- Photodegradation of benzydamine: Phototoxicity of an isolated photoproduct on erythrocytes
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Benzydamine hydrochloride (Tantum, 1) is a photoallergic and phototoxic anti-inflammatory and analgesic agent. This drug is photolabile under aerobic and anaerobic conditions. Irradiation of a methanol solution of benzydamine under oxygen or argon at 300 nm affords 5-hydroxybenzydamine (2) and 2-β- dimethylaminopropyl-1-benzylindalolin-3-one (3) as the main isolated and spectroscopically identified photoproducts. A radical intermediate was evidenced by thiobarbituric acid that was used as a radical sonde, as well as by the dimerization of cysteine. Erythrocyte lysis phososensitized by 1, 2, and 3 was investigated.
- Vargas,Rivas,Machado,Sarabia
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p. 371 - 372
(2007/10/02)
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- ACTION OF NITROUS ACID ON N-SUBSTITUTED-ISATINIC ACIDS. DISPROPORTIONATION TO INDAZOLOLS.
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By reacting N-substituted-2-isatinic acids with nitrous acid, indazolols, N-nitroso-N-substituted anthranilic acids and the esters of said acids with the above mentioned indazolols were obtained through disproportionation of the N-nitroso-N-substituted-isatinic acids.
- Baiocchi,Leandro,Picconi, Giuseppe
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p. 3651 - 3652
(2007/10/02)
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- Reactions of Hydrazides and Hydrazones with n-Butyl-lithium
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Aromatic hydrazides give indazol-3(2H)-ones in good yield when treated with 3 equivalents of n-butyl-lithium; aliphatic and heterocyclic hydrazides afford the corresponding aldehydes under the same conditions.
- Barton, Derek H. R.,Lukacs, Gabor,Wagle, Dilip
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p. 450 - 452
(2007/10/02)
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