4722-81-0Relevant articles and documents
Synthesis method of chronic granulocytic leukemia treating medicinal intermediate
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Paragraph 0016; 0119; 0024, (2018/09/08)
The invention relates to a synthesis method of a chronic granulocytic leukemia treating medicinal intermediate. The synthesis method comprises the following steps: (a), dissolving trichloroacetaldehyde hydrate by using water, sequentially adding an aqueous solution of anhydrous sodium sulfate, a hydrochloric acid solution of 3, 4-dimethoxyaniline and an aqueous solution of hydroxylamine hydrochloride, filtering and drying to obtain a compound 2; (b), mixing the compound 2 and polyphosphoric acid to obtain a compound 3; (c), dissolving the compound 3 and rhodanine by using pyridine, and dryingto obtain a compound 4; (d), mixing the compound 4 and a KOH solution, heating to 40-60 DEG C, reacting while stirring, and drying to obtain a compound 5. By the synthesis method, synthesis of a key intermediate of an indirubin derivative can be achieved, the yield and the purity are relatively high, and industrial batch production is facilitated.
Method for synthesizing drug for treating chronic granulocytic leukemia
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Paragraph 0018; 0021; 0027, (2018/09/11)
The invention relates to a method for synthesizing a drug for treating chronic granulocytic leukemia. The method comprises the following steps: (a) dissolving a chloral hydrate with water, sequentially adding an aqueous solution of anhydrous sodium sulfate, a hydrochloric solution of 3,4-dimethoxyaniline and an aqueous solution of hydroxylamine hydrochloride, and performing filtering and drying, so as to obtain a compound 2; (b) mixing the compound 2 with polyphosphoric acid, so as to obtain a compound 3; (c) dissolving the compound 3 and rhodanine with pyridine, and carrying out drying, so asto obtain a compound 4; (d) mixing the compound 4 with a KOH solution, then, heating the temperature of the mixture to 40 DEG C to 60 DEG C, carrying out a reaction with stirring, and carrying out drying, so as to obtain a compound 5; (e) mixing the compound 5 with aniline, then, carrying out a reaction with stirring at the temperature of 100 DEG C to 150 DEG C under nitrogen protection, and carrying out drying, so as to obtain a compound 6; (f) heating the temperature of polyphosphoric acid to 100 DEG C to 150 DEG C, adding the compound 6 under the condition of continuous stirring, carryingout a reaction, and carrying out purification, thereby obtaining the drug. Thus, indirubin derivatives can be synthesized and have relatively high yield and purity, and the industrialized mass production is facilitated.
Synthesis method for final intermediate of chronic granulocytic leukemia drug
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Paragraph 0017; 0020; 0026, (2018/09/12)
The invention relates to a synthesis method for a final intermediate of a chronic granulocytic leukemia drug. The method comprises the steps of: (a) dissolving a trichloracetic aldehyde hydrate in water, then adding an aqueous solution of anhydrous sodium sulfate, a hydrochloric acid solution of 3, 4-dimethoxyaniline and an aqueous solution of hydroxylamine hydrochloride in order, and conducting filtering and drying to obtain a compound 2; (b) mixing the compound 2 with polyphosphoric acid to obtain a compound 3; (c) dissolving the compound 3 and rhodanine in pyridine, and performing drying toobtain a compound 4; (d) mixing the compound 4 with a KOH solution, then performing heating to 40-60DEG C, carrying out stirring reaction, and performing drying to obtain a compound 5; and (e) mixingthe compound 5 with aniline, then carrying out stirring reaction at 100-150DEG C under nitrogen protection; and performing drying to obtain a compound 6. The method provided by the invention can realize synthesis of indirubin derivative intermediates with high yield and purity, and is conducive to industrial batch production.
A novel strategy to the synthesis of 4-anilinoquinazoline derivatives
Wang, Zheng,Wang, Cuiling,Sun, Yanni,Zhang, Ning,Liu, Zhulan,Liu, Jianli
, p. 906 - 913 (2014/01/23)
A novel approach to prepare 4-anilinoquinazoline derivatives based on the transformation of indoline-2,3-dione to formamidine was developed. The processes with this approach are simple, efficient, and environmentally friendly. The efficiency of this approach was evaluated by synthesizing 17 4-anilinoquinazolines and comparing the obtained yields with those achievable through conventional synthetic methods. It was the first time that compounds 8d, 8e, 8h, and 13b-f were synthesized. The characteristics of the IR and the UV spectra of these compounds and the effects of their substituents on the spectra were observed.
Synthesis and biophysical evaluation of arylhydrazono-1H-2-indolinones as β-amyloid aggregation inhibitors
Campagna, Francesco,Catto, Marco,Purgatorio, Rosa,Altomare, Cosimo D.,Carotti, Angelo,De Stradis, Angelo,Palazzo, Gerardo
scheme or table, p. 275 - 284 (2011/02/27)
A series of isatin-3-arylhydrazones were synthesized and evaluated in vitro as inhibitors of Aβ1-40 aggregation using a thioflavin T fluorescence method. An exploration of the effects on Aβ1-40 aggregation of a number of diverse subs
A new approach to methoxyisatins leading to the total synthesis of ophiuroidine and other hydroxytryptanthrins
Mason, Jeffrey J.,Janosik, Tomasz,Bergman, Jan
experimental part, p. 3642 - 3648 (2010/03/05)
A new method for the preparation of methoxyisatins from the corresponding methoxyanilines is described. The resulting methoxyisatins were used in the syntheses of several methoxytryptanthrin compounds. The natural product ophiuroidine (4,8,9-trihydroxytry
Combinatorial optimization of isatin-β-thiosemicarbazones as anti-poxvirus agents
Pirrung, Michael C.,Pansare, Sunil V.,Das Sarma, Koushik,Keith, Kathy A.,Kern, Earl R.
, p. 3045 - 3050 (2007/10/03)
Novel strategies are required to combat pox virus infections, whether caused by escape of viruses such as monkeypox from indigenous areas or intentional release of smallpox. Anti-smallpox drugs with a unique mode of antiviral action, inhibition of transcription termination, were known but not therapeutically useful. Using a combinatorial method, variants of the basic isatin-β-thiosemicarbazone structure were prepared and examined for cytotoxicity and antiviral activity in vaccinia virus- and cowpox virus-infected human cells. Potent and much more selective N-aminomethyl-isatin-β- thiosemicarbazones were discovered.
Synthesis of Dopamines Labelled with 13C in the α- or β-Side Chain Position and Their Application to Structural Studies on Melanins by Solid-State NMR Spectroscopy
Crescenzi, Orlando,Kroesche, Christoph,Hoffbauer, Wilfried,Jansen, Martin,Napolitano, Alessandra,et al.
, p. 563 - 568 (2007/10/02)
Solid-state NMR spectroscopy was applied to the analysis of melanins prepared by peroxidase-H2O2 oxidation of dopamines specifically 13C labelled in the α- or β-side chain positions.A surprisingly diverse pattern of signals indicated the presence of uncyclized dopamine and noradrenaline-derived units, in addition to indole and carbonyl carbon atoms.These structural features, coupled with the results obtained from elemental analysis of dopamine melanin samples prepared under different conditions, point to a pigment formation process more complex than previously believed. - Key Words: CP-MAS NMR Spectroscopy / Melanin / Oxidative phenolic coupling / Quinone methides / Labelled compounds, 13C / Dopamines / Enzymes
PHOTO-OXIDATION OF 5,6-DIHYDROXYINDOLES
d'Ischia, Marco,Prota, Giuseppe
, p. 407 - 410 (2007/10/02)
The photo-oxidative behaviour of some 5,6-dihydroxyindoles (1-6) in organic solvents with Pyrex-filtered UV light has been investigated.In methanol, all the indoles exhibited a marked tendency to undergo photodecomposition giving very complex mixtures of products.In the case of 5,6-dimethoxyindole, 5, work-up of the reaction mixture led to isolation of two main photo-oxygenation products which were identified as the isatin 7 and the ring-opened derivative 8 by spectral analysis.The use of acetone as solvent markedly altered the reaction cource, causing cleavage of the C2-C3 bond in all the indoles examined, including the parent ring system, to give N-formylanthranilic acid in good yields.
The Synthesis of the Dimethoxyisatins
Taylor, A.
, p. 4154 - 4171 (2007/10/02)
Preparations of all 6 dimethoxyisatins are described.The methods of synthesis of these compounds from anilines have been compared, the route via the 3-(methylthio)oxindoles giving, in general, the best yield.These isatins are strikingly different in colou
