- High-purity L-sunitinib malate preparation method
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The present invention discloses a high-purity L-sunitinib malate preparation method, which comprises the following reaction route defined in the specification, wherein the step a comprises that a B5 compound and 5-fluoroindol-2-one are subjected to an Aldol condensation reaction to obtain a sunitinib free base (B6 compound), the step b comprises that the B6 compound and L-malic acid are subjected to a salt forming reaction to obtain the L-sunitinib malate, and the step a and the step b are performed in a dark place. According to the present invention, the HPLC purity of the prepared L-sunitinib malate can achieve more than 99.8%, the single impurity content can be controlled at less than 0.1%, and the quality difficulty of the application of the L-sunitinib malate in the preparation is effectively solved.
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Paragraph 0034; 0041; 0042
(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 24; 25
(2010/12/26)
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- Method of synthesizing indolinone compounds
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Disclosed are methods of preparing pyrrole compounds of formula 14 and indolinone compounds of formula 1 via a synthetic route wherein the amide sidechain on the pyrrole moiety is attached prior to pyrrole formation. The compounds 14 produced by the methods herein are useful in the synthesis of compounds of formula 1, which are useful in the treatment of abnormal cell growth, such as cancer.
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Page/Page column 16
(2010/02/15)
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- Synthesis of [18F]SU11248, a new potential PET tracer for imaging cancer tyrosine kinase
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N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-[18F]fluoro-2-oxo-1, 2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide, a new potential positron emission tomography tracer for imaging cancer tyrosine kinase, has been prepared by the nucleophilic substitution of the nitro-precursor N-[2-(diethylamino)ethyl]-5-[(Z)-(5-nitro-2-oxo-1,2-dihydro-3H- indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide with K 18F/Kryptofix 2.2.2 followed by a simple chromatography methodology combined solid-phase extraction with high-performance liquid chromatography purification procedures in 15-25% radiochemical yields.
- Wang, Ji-Quan,Miller, Kathy D.,Sledge, George W.,Zheng, Qi-Huang
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p. 4380 - 4384
(2007/10/03)
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- Method for catalyzing amidation reactions
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The invention provides a method of preparing a compound of formula 2 wherein R1 and R6 are as defined herein, by a catalytic amidation process in the presence of added carbon dioxide. The inventive methods show surprising rate enhancement relative to the corresponding uncatalyzed reaction.
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Page/Page column 12
(2008/06/13)
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- Amidations Using N,N′-Carbonyldiimidazole: Remarkable Rate Enhancement by Carbon Dioxide
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Carbon dioxide catalyzes the reaction of imidazolides with amines to form amides. A substantial rate enhancement is observed in the presence of CO 2 compared to the CO2-free case. The scope and limitations of this reaction are discussed.
- Vaidyanathan, Rajappa,Kalthod, Vikram G.,Ngo, Duc P.,Manley, Jerad M.,Lapekas, Sean P.
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p. 2565 - 2568
(2007/10/03)
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- Early amidation approach to 3-[(4-amido)pyrrol-2-yl]-2-indolinones
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A new synthesis of 3-[(4-amido)pyrrol-2-yl]-2-indolinones has been developed, where the amide side chain was installed prior to pyrrole formation. This strategy precludes the need to use any coupling reagents to install the amide side chain. This process includes a zinc-free alternative to the Knorr pyrrole synthesis.
- Manley, Jerad M.,Kalman, Monica J.,Conway, Brian G.,Ball, Cynthia C.,Havens, Jeffrey L.,Vaidyanathan, Rajappa
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p. 6447 - 6450
(2007/10/03)
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