- Industrial synthesis method of rilpivirine and intermediate compound
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The invention discloses an industrial synthesis method of rilpivirine. A compound as shown in a formula I and compound hydrochloride as shown in a formula VI react to obtain rilpivirine. The invention further discloses an intermediate compound as shown in the formula I and a synthesis method of the intermediate compound. Compared with the prior art, the synthesis method is simple to operate, mild in condition, high in yield and purity and suitable for industrial production.
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Paragraph 0028; 0041; 0042; 0068; 0077; 0086; 0095; 0104
(2017/10/07)
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- Pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and preparation method and application thereof
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The invention provides pyrimidine heterocyclic compounds, pyrimidine heterocyclic compound salts, and a preparation method and application thereof. According to the pyrimidine heterocyclic compounds provided by the invention, specific Rq is selected, so that the obtained compounds have favorable drug resistance and long half life when being used as the medicine for treating or preventing HIV. The compounds have the advantages of high activity, low toxicity and high stability.
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Paragraph 0123; 0130; 0131; 0132
(2017/07/26)
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- 4-[ (4-chloro-2-pyrimidinyl) amino] phenyl nitrile preparation method
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The invention discloses a new preparation method of 4-[(4-chlorine-2-pyrimidyl)amino] cyanophenyl. The preparation method comprises the steps of carrying out a reaction on N-guanidine cyanophenyl and NN,-dimethyl amino acrylate to generate II, and then carrying out chlorination on equivalent phosphorus oxychloride to generate a target product. By adopting the preparation method, the yield and the quality of the product can be improved; the cost is reduced, and the method is simple and convenient to operate, and suitable for a synthetic route of rilpivirine bodbody in industrial production.
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Paragraph 0032-0034
(2020/05/01)
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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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Paragraph 0040; 0058
(2014/09/30)
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- PROCESS FOR RILPIVIRINE
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The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
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Paragraph 0081
(2014/08/19)
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- RILPIVIRINE HYDROCHLORIDE
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The present invention provides a novel process for the preparation of rilpivirine. The present invention also provides a novel process for the preparation of rilpivirine hydrochloride. The present invention further provides a rilpivirine hydrochloride monohydrate, process for its preparation and pharmaceutical compositions comprising it.
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Paragraph 0084
(2014/12/09)
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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 8; 9
(2013/03/28)
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- PROCESS FOR RILPIVIRINE
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The present invention provides a novel process for the preparation of 4-(4-hydroxypyrimidin-2-ylamino)benzonitrile. The present invention also provides a novel process for the preparation of 4-iodo-2,6-dimethyl benzenamine. The present invention further provides an improved process for the preparation of rilpivirine. The present invention further provides a tosylate salt of rilpivirine, process for its preparation and pharmaceutical compositions comprising it.
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Page/Page column 7-8
(2012/11/13)
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- Evolution of anti-HIV drug candidates. Part 3: Diarylpyrimidine (DAPY) analogues
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The synthesis and anti-HIV-1 activity of a series of diarylpyrimidines (DAPYs) are described. Several members of this novel class of non-nucleoside reverse transcriptase inhibitors (NNRTIs) are extremely potent against both wild-type and a panel of clinically significant single- and double-mutant strains of HIV-1.
- Ludovici, Donald W.,De Corte, Bart L.,Kukla, Michael J.,Ye, Hong,Ho, Chih Y.,Lichtenstein, Mark A.,Kavash, Robert W.,Andries, Koen,De Bethune, Marie-Pierre,Azijn, Hilde,Pauwels, Rudi,Lewi, Paul J.,Heeres, Jan,Koymans, Lucien M.H.,De Jonge, Marc R.,Van Aken, Koen J.A.,Daeyaert, Frederik F.D.,Das, Kalyan,Arnold, Edward,Janssen, Paul A.J.
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p. 2235 - 2239
(2007/10/03)
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