55453-89-9Relevant academic research and scientific papers
Preparation method of olopatadine hydrochloride
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Paragraph 0039-0041, (2021/11/10)
The method comprises the following steps: [3 - (dimethylamino) propyl] triphenylphosphonium bromide hydrobromide is added into tetrahydrofuran. The sodium hydride and dimethyl sulfoxide are added 11 - oxo -6, 11 - dihydrodibenzo [b, e] oxazepine -2 - acetic acid and stirred until the reaction system forms a black brown suspension reaction. The reaction solution is quenched by a mixed solution of purified water and tetrahydrofuran, and then the aqueous phase is treated with a mixed solvent of hydrochloric acid and n-butanol. The olopatadine hydrochloride is stirred and added with hydrochloric acid to form a white turbid liquid, and then is filtered through stirring after stirring, and is dried to obtain olopatadine hydrochloride, and the prepared oxalolopatadine hydrochloride is high in yield and short in reaction route.
A process for the preparation of olopatadine hydrochloride
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Paragraph 0053; 0054, (2016/10/08)
The invention relates to a method for preparing a compound, namely, olopatadine hydrochloride. The method specifically comprises the following steps: by taking 2-chloromethyl methyl benzoate and methyl 4-hydroxyphenylacetate as initial raw materials, performing etherification, hydrolysis and cyclization, further performing wittig reaction, and salifying, thereby synthesizing olopatadine hydrochloride. The process is gentle in process reaction condition, acetic anhydride is adopted to replace polyphosphoric acid, a hydrochloric acid organic solvent is adopted to effectively split Z/E type olopatadine so as to obtain olopatadine hydrochloride, conversion of Z/E configuration is effectively achieved after an E configuration byproduct is treated by using concentrated hydrochloric acid, the yield of olopatadine hydrochloride is increased, the product purity is good, and the feasibility of industrialization production is greatly improved.
IMPROVED PROCESS FOR LL-[(Z)-3-(DIMETHYLAMINO)PROPYIIDENEL-6-LL- DIHYDRODIBENZ[B,EL OXEPIN-2-ACETICACID
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Page/Page column 20-21, (2011/11/01)
The present invention relates to an improved process for the preparation of 11- [(Z)-3-(dimethylamino)propylidene]-6, 11 -dihydrodibenzo[b,e]oxepin-2-aceticacid compound of formula- 1 and its pharmaceutically acceptable salts.
2-(4-METHOXYCARBONYLMETHYLPHENOXYMETHYL)BENZOIC ACID METHYL ESTER AND METHOD FOR PRODUCING THE SAME
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Page/Page column 8-9, (2009/06/27)
Dibenzoxepinacetic acid useful as an intermediate for pharmaceutical products can advantageously be produced by way of a method for producing methyl 2-(4-methoxycarbonylmethylphenoxymethyl)benzoate comprising a reaction of methyl 2-chloromethylbenzoate with methyl 4-hydroxyphenylacetate.
TERTIARY ALKYL ESTER OF OXODIBENZOXEPIN ACETIC ACID
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Page/Page column 10, (2009/07/17)
A tertiary alkyl ester represented by Formula (2): wherein R1 and R2 each independently represent a C1-4 alkyl group, and a method for producing the same.
Polymorphic forms of olopatadine hydrochloride and methods for producing olopatadine and salts thereof
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Page/Page column 23, (2008/06/13)
The present invention provides a novel polymorphic form of olopatadine hydrochloride ([(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid hydrochloride), a selective histamine H1-receptor antagonist that is used for the treatment of ocular symptoms of seasonal allergic conjunctivitis. The present invention also provides novel methods for producing olopatadine on a large scale, and in a manner that is cost effective, provides a low level of impurities and eliminates the need to use the costly and dangerous base, butyllithium, which is used in prior art reactions for making olopatadine. The present invention further provides novel processes for carrying out a large scale production of 3-dimethylaminopropyltriphenylphosphonium bromide and its corresponding hydrobromide salt, which are employed in the production of olopatadine, and pharmaceutically acceptable salts of olopatadine.
Dibenzoxepinone hydroxylamines and hydroxamic acids: Dual inhibitors of cyclooxygenase and 5-lipoxygenase with potent topical antiinflammatory activity
Hamer, R. Richard L.,Tegeler, John J.,Kurtz, Ellen S.,Allen, Richard C.,Bailey, Steven C.,Elliott, Mary Ellen,Hellyer, Luther,Helsley, Grover C.,Przekop, Penelope,Freed, Brian S.,White, John,Martin, Lawrence L.
, p. 246 - 252 (2007/10/03)
Hydroxylamine and hydroxamic acid derivatives of a known nonsteroidal antiinflammatory dibenzoxepine series display both cyclooxygenase (CO) and 5- lipoxygenase (5-LO) inhibitory properties. Many of these new dual CO/5-LO inhibitors also exhibit potent topical antiinflammatory activity in the arachidonic acid-induced murine ear edema model. On the basis of their promising profile of in vitro and in vivo activities, hydroxamic acids 24h, 3-(6,11-dihydro-11-oxodibenz[b,e]oxepin-2-yl)-N-hydroxy-N-methylpropanamide (HP 977), and 25, 3-(6,11-dihydrodibenz[b,e]oxepin-2-yl)-N-hydroxy-N- methylpropanamide (P10294), were selected as developmental candidates for the topical treatment of inflammatory skin disorders.
Dibenz[b,e]oxepin compounds
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, (2008/06/13)
Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
