- Malic acid lin's preparation method
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The present invention relates to a sunitinib malate preparation method, wherein particularly 2,4-dimethyl-5-aldehyde-1H-pyrrole-3-carboxylic acid is adopted as a starting raw material, carboxyl activation with carbonyl diimidazole is performed, the obtained material and N, N-diethylethylenediamine are subjected to condensation under catalysis of 1-hydroxybenzotriazole to obtain an intermediate 1, the intermediate 1 and 5-fluoro-2-oxindole react to obtain sunitinib, and the sunitinib and malic acid are directly subjected to salifying without separation so as to obtain the target product. The method of the present invention has characteristics of easy operation, high yield and high product purity, and is suitable for industrial production.
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Paragraph 0029; 0034; 0036; 0041; 0043
(2019/06/12)
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- Method for preparing sunitinib
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The invention relates to a method for preparing sunitinib. According to the method, the sunitinib is prepared by adopting a one-pot method. The method comprises the steps of reacting a starting material 5-fluoroindole-2-ketone with 4-dimethyl-5-aldehyde-1H-pyrrole-3-carboxylic acid to generate an intermediate 5-[(5-fluoro-2-oxo-1,2-dihydro-3H-indole-3-subunit) methyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid; and directly reacting the generated intermediate with N,N-diethylethylenediamine without separating the intermediate to form the sunitinib.
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Paragraph 0032; 0051; 0054; 0060; 0062
(2019/04/09)
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- Method for recovering and utilizing byproduct of chlorination of phosphorus pentachloride
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The invention relates to a technology for comprehensively utilizing the byproduct of chlorination of phosphorus pentachloride, and mainly relates to a post treatment, which scientifically utilizes the excess phosphorus pentachloride reagent. The byproduct is converted into an organic synthesis reagent with a wide application range. The wastes are converted into a valuable resource. The discharge of waste water, waste gas, and waste solid is reduced. The obtained reagent is an excellent active reagent, which is widely used in the chemical industry, pharmacy industry, and material industry. The production cost is reduced, and the environment is protected.
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Paragraph 0034-0035
(2017/08/28)
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- PROCESS FOR THE PREPARATION OF N-[2-DIETHYLAMINO)ETHYL]-5-[(5-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE)METHYL]-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXAMIDE
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The present invention relates to processes for the preparation of N-[2-(Diethylamino) ethyl]-5-[ (5-fluoro-1, 2 -dihydro-2-oxo-3H-indol-3-ylidene) methyl] -2, 4-dimethyl-I H-pyrrole- 3 -carboxamide of formula (VI).
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Page/Page column 27; 28
(2010/12/26)
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- NOVEL SALTS OF SUNITINIB
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The present invention relates to novel pharmaceutically acceptable salts of sunitinib, to processes for their preparation and to pharmaceutical compositions containing them.
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Page/Page column 16; 17
(2010/05/14)
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