CAS: 112885-41-3; 4-Amino-5-Chloro-2-Ethoxy-N-((4-(4-Fluorobenzyl)Morpholin-2-yl)Methyl)Benzamide

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(Rs)-4-(Tert-Butoxy-Carbonyl-Amino)-5-Chloro-2-Ethoxy-N-{[4-(4-Fluoro-Benzyl)-2-Morpholinyl]Methyl}-Benzamide置于盐酸体系中,用 水 用作溶剂,化学反应 3.0H,以100%的收率获得莫沙必利
参考文献: Process For The Synthesis Of Mosapride[fr] Procede De Synthese D'Un Derive Benzamide
标题: Process For The Synthesis Of Mosapride[fr] Procede De Synthese D'Un Derive Benzamide

专利信息

专利号:WO-03106440-A3
优先权日:2002-06-13
标题 :PROCESS FOR THE SYNTHESIS OF A BENZAMIDE DERIVATIVE
发明人：VUKICS KRISZTINA; FISCHER JANOS; LEVAI SANDOR; ERDELYI PETER
权利人:RICHTER GEDEON VEGYESZET; VUKICS KRISZTINA; FISCHER JANOS; LEVAI SANDOR; ERDELYI PETER
摘要:This invention relates to a process for the synthesis of mosapride citrate represented by the formula (I) and having the chemical name: (R, S) -4-amino-5-chloro-2-ethoxy-N - {- citrate dihydrate 4- (4-fluoro-benzyl) -2-morpholinyl] methyl} benzamide. The method of this invention comprises reacting the compound represented by formula (II) with di-tert-butyl-dicarbonate in an alcohol in the presence of a base; ethylating the product obtained in an inert solvent in the presence of a base; then hydrolyzing the compound obtained with an alkyl hydroxide and neutralizing the salt obtained with an acid. This process then consists in chlorinating the product obtained, then reacting the compound obtained represented by formula (VI) with the compound represented by formula (VII) in which BOC denotes a protective group of tert-butoxy-carbonyl; and removing the protecting group from the compound obtained represented by the formula (VIII) in which BOC is as defined above. It is then a question of preparing the mosapride base, and optionally of producing, by means of an acid and preferably citric acid, a pharmaceutically acceptable salt, preferably the mosapride citrate dihydrate represented by the formula (I ).

专利号:US-7211590-B2
优先权日:2002-08-01
标 题:Nitrosated proton pump inhibitors, compositions and methods of use
发明人：FANG XINQIN; GARVEY DAVID S; LETTS L GORDON
权利人:NITROMED INC
摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated proton pump inhibitor compound, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.

专利号:US-2024051897-A1
优先权日:2022-07-26
标题:Synthesis of complex 15n-labeled molecules
发明人：DORSHEIMER JULIA; ROVIS TOMISLAV
权利人:UNIV COLUMBIA
摘要:Methods for conversion of a broad range of amines to their 15N isotopic counterparts and the compounds produced thereby.

专利号:US-2008280855-A1
优先权日:2005-06-22
标 题 :Process For the Production of Intermediates For the Preparation of Tricyclic Benzimidazoles
发明人：CHIESA MARIA VITTORIA; PALMER ANDREAS; BUHR WILM; ZIMMERMANN PETER JAN; BREHM CHRISTOF; SIMON WOLFGANG-ALEXANDER; POSTIUS STEFAN; KROMER WOLFGANG; ZANOTTI-GEROSA ANTONIO
权利人:NYCOMED GMBH
摘要:The invention relates to a process for the synthesis of compounds of the formula 1-a and compounds of the formula 1-b. n n n n n n n n n n The compounds of the formula 1-a and the compounds of the formula 1-b, in which the substituents R1, R2, R3, and Ar have the meanings indicated in the description, are valuable intermediates for the preparation of pharmaceutically active compounds.

专利号:WO-0054773-A1
优先权日:1999-03-12
标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
发明人：GARVEY DAVID S
权利人:NITROMED INC; GARVEY DAVID S
摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

专利号:US-10434098-B2
优先权日:2015-06-02
标 题 :Deuterated dehydrophenylahistin compounds and preparation method thereof and use thereof in preparation of anti-tumor drugs
发明人：LI WENBAO; SUN TIANWEN; WANG SHIXIAO; ZHAO JIANCHUN; CAI BING; GUAN HUASHI
权利人:MARINE BIOMEDICAL RES INST QINGDAO CO LTD
摘要:Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehydrophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.