- Preparation process of Rupatadine
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The invention discloses a rupatadine preparation process, which comprises: S1, preparing methyl 5-methylnicotinate; S2, preparing 5-methyl-3-pyridinemethanol; S3, preparing 3-methyl-5-chloromethylpyridine hydrochloride; and S4, preparing rupatadine. According to the present invention, the preparation process has advantages of low cost, mild reaction condition, simple operation, low requirement onequipment, good product purity and high yield, and is suitable for large-scale industrial production.
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Paragraph 0057; 0063; 0069; 0075; 0081; 0087; 0093; 0096
(2017/08/28)
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- An improved process for the preparation of Rupatadine Fumarate
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The present invention provides an improved process for the preparation of Rupatadine Fumarate of Formula-1 resulting product which is substantially free from di-alcohols, dimer and quaternary impurities.
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- NOVEL CRYSTALLINE FORM OF RUPATADINE FREE BASE
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The present invention relates to a novel crystalline form of rupatadine free base, process for its preparation and to a pharmaceutical composition containing it. In accordance with the present invention rupatadine is suspended in n-hexane, n-heptane, cyclohexane, diethyl ether or diisopropyl ether, stirred for at least 1 hour, filtered the solid and dried to give crystalline rupatadine form-B. The isolation of novel rupatadine free base as crystalline form-B may be useful as a purification of rupatadine or a salt thereof.
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Page/Page column 3
(2009/08/16)
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- Expedient synthesis of rupatadine
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Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF), has been synthesized in 91% overall yield. Copyright Taylor & Francis Group, LLC.
- Agarwal, Rajendra,Bhirud, Shekhar Bhaskar,Bijukumar, Gopinathenpillai,Khude, Gopal Dnyandev
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p. 122 - 127
(2008/03/14)
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- A NOVEL CRYSTALLINE FORM OF RUPATADINE FREE BASE
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The present invention relates to a novel crystalline form of rupatadine free base, process for its preparation and to a pharmaceutical composition containing it. In accordance with the present invention rupatadine is suspended in n-hexane, n-heptane, cyclohexane, diethyl ether or diisopropyl ether, stirred for at least 1 hour, filtered the solid and dried to give crystalline rupatadine form-B. The isolation of novel rupatadine free base as crystalline form-B may be useful as a purification of rupatadine or a salt thereof.
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Page/Page column 5-6
(2010/11/24)
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- A PROCESS FOR THE PREPARATION OF RUPATADINE
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Rupatadine is synthesized by phase transfer catalysed N-alkylation of Desloratadine in biphasic solvent system using aqueous alkali by reaction of a compound of formula (I), with Desloratadine at temperature up to 500C , wherein solvent selected is water immiscible organic solvent. Rupatadine is further converted to Rupatadine fumarate by reaction of Rupatadine in ketonic solvent with an alcoholic solution of fumaric acid.
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Page/Page column 6-7
(2008/06/13)
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- 8-chloro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidyliden]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,]pyridine
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The present invention relates to 8-chloro-11-[1-[(5-methyl-3-pyridyl)methyl]-4-piperidyliden]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, to a process for its preparation and to pharmaceutical compositions containing it. This compound is a dual PAF antagonist and antihistamine.
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- [(3-Pyridylalkyl)piperidylidene]benzocycloheptapyridine derivatives as dual antagonists of PAF and histamine
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A series of [(3-pyridylalkyl)piperidylidene]- and (nicotinoylpiperidylidene)benzocycloheptapyridine derivatives, Ia,b, were prepared and evaluated for PAF antagonist and H1 antihistamine activity. PAF antagonist activity was investigated by the in vitro PAF-induced platelet aggregation assay (PPA) and the in vivo PAF-induced hypotension test in rats (PH) and mortality test in mice (PM). For the evaluation of H1 antihistamine activity, the in vitro histamine-induced contraction of the guinea-pig ileum assay (HC) and the in vivo histamine-induced hypotension test (HH) in normotensive rats were used. The potential antiallergic activity of the compounds was evaluated using the active anaphylactic shock test in mice. These compounds are structurally related to loratadine (1) and were generated by replacement of the ethoxycarbonyl group of 1 with substituted 3- pyridylmethyl and nicotinoyl moieties. Both anti-PAF and H1 antihistamine activities have shown a high dependence on the exact nature and position of the substituent in the pyridine ring. Optimum structure 19 (UR-12592) incorporating a (5-methyl-3-pyridyl)methyl radical displayed an unique dual activity inhibiting both PAF-induced effects (PPA, IC50 = 3.7 μM; PH, ID50 = 0.44 mg/kg iv; PM, ID50 = 1.9 mg/kg po) and histamine-induced effects (HC, IC50 = 3.9 nM; HH, ID50 = 1.4 mg/kg iv). Furthermore, 19 was highly active in the passive cutaneous anaphylactic shock in rats (ID50 = 1.2 mg/kg po) and strongly protected mice and rats from mortality induced by endotoxin (ID50 = 1.2 and 0.5 mg/kg iv, respectively). Compound 19 showed itself to be devoid of CNS depressant effects, neither modifying spontaneous motor activity nor prolonging barbiturate-sleeping time in mice at a dose of 100 mg/kg po, and is now under development.
- Carceller,Merlos,Giral,Balsa,Almansa,Bartroli,Garcia- Rafanell,Forn
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p. 2697 - 2703
(2007/10/02)
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