- Method for preparing high-purity ribavirin intermediate by one-pot method (by machine translation)
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The invention relates to the technical field of chemical medicine, in particular to a method for preparing a high-purity ribavirin intermediate by a one-pot method. The method comprises the following steps: (1) replacing the compound I with the compound II to obtain the reaction liquid of the compound III. (2) Acrylamide was added to III reaction liquid of the compound, and the reaction liquid of compound IV was obtained under Heck reaction conditions. (3) In the reaction solution of Compound IV, activated carbon is first added for decolorization treatment, and then a poor solvent is added for crystallization to obtain a white compound IV, i.e. a ripe intermediate. The method for preparing the high-purity ribavirin intermediate by one-pot method is scientific, reasonable, simple and feasible, improves product purity and yield, and is suitable for large-scale production. (by machine translation)
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- PROCESS FOR THE PREPARATION OF RILPIVIRINE
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The present invention relates to a new process of preparation of Rilpivirine, or a pharmaceutically acceptable salt thereof. Another aspect of the invention concerns compounds of formulae II and III: and their salts thereof, and their use for the preparation of Rilpivirine or a suitable salt thereof.
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- RILPIVIRINE PROCESS
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Disclosed is process for the preparation of a key Rilpivirine intermediate namely, (E)-4-(2-cyanoethenyl)-2,6-dimethylphenylamine hydrochloride (II) by a process comprising reaction of the tetrafluoroborate salt of the diazonium ion of 2,6-dimethyl-4-amin
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- RILPIVIRINE HYDROCHLORIDE
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As used herein the term "room temperature" refers to a temperature of about 25°C to about 35°C. According to one aspect of the present invention, there IS provided a novel process for the preparation of rilpivirine, which comprises: a) condensing the (E)-3-( 4-amino-3,5-dimethylphenyl)acrylonitrile hydrochloride with 4-( 4-chloropyrimidin-2-ylamino )benzonitrile m the presence of Nmethylpyrrolidone; b) heating the contents obtained in step (a) at about 75 to 95°C to obtain a solution; c) cooling the solution obtained in step (b) at below 35°C; d) adding water to the reaction mass; and e) isolating rilpivirine. The reaction in step (b) may preferably be heated to 100 to 110°C. Step (c) may preferably be carried out at room temperature. Rilpivirine may be isolated in step (e) by the methods known such as Filtration or centrifugation.
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Page/Page column 10; 11
(2013/03/28)
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