CAS: 54739-18-3; Fluvoxamine

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5-methoxy-1-[4-(trifluoromethyl)phenyl]pentan-1-one 2-chloroethanamine hydr°Chloride 3C6H4CN4-CF3C6H4CN 4-Methoxy-1-bromobutane

5-甲氧基-1-[4-(三氟甲基)苯基]-1-戊酮置于盐酸羟胺,Sodium Acetate,Potassium Hydroxide体系中,用 乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 3.0H,反应生成 氟提肟氨
参考文献:通过引入卤素原子调整已知药物的活性,Sert 配体-氟西汀和氟伏沙明的案例研究
标题:通过引入卤素原子调整已知药物的活性,Sert 配体-氟西汀和氟伏沙明的案例研究
摘要:作用于血清素转运蛋白 (Sert) 的选择性血清素再摄取抑制剂 (Ssri) 是处方最广泛的抗抑郁药物之一.所有五种获批的 Ssri 都含有氟或氯原子,并且描述它们与较重卤素(即溴和碘)类似物的报告数量有限.为了阐明卤素原子在 Ssris 与 Sert 结合中的作用,我们设计了一系列 22 种氟西汀和氟伏沙明类似物,它们被氟,氯,溴和碘原子取代,它们在苯环上的排列不同.获得的生物活性数据,得到了全面的计算机支持结合模式分析,允许识别卤素键相互作用的两个伙伴:E493 和 T497 的骨架羰基氧原子.此外,发现具有较重卤素原子的化合物通过明显不同的结合模式与 Sert 结合,这一结果未在别处介绍.对制备的 Xsar 集的后续分析表明,E493 和 T497 参与形成的卤键数量最多.xsar 库分析导致合成了两种最活跃的化合物(3,4-Dicl-氟西汀42,Sert K I = 5 Nm 和 3
DOI:10.1016/j.Ejmech.2021.113533

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-2003083352-A1
优先权日:2000-07-31
标 题 :Synthesis of imidazole intermediates
发明人：HELAL CHRISTOPHER J
权利人:PFIZER
摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:WO-2015194928-A1
优先权日:2014-06-17
标 题:Method for the isolation and synthesis of 3-(1´, 1´- dimethylallyl)-herniarin, as well as (e)-3-(1´,1´-dimethyl-3´nitro-allyl-herniarin, from casimiroa pubescens, and use thereof as an antidepressant
发明人：MARTÃ?NEZ VÃ?ZQUEZ MARIANO; ESTRADA REYES ROSA; UBALDO SUÃ?REZ DENISSE; DE LA ROSA SIERRA ROBERTO
权利人:UNIV NAC AUTÓNOMA DE MÉXICO
摘要:The invention relates to the compounds 3-(1´,1´ -dimethylallyl)-herniarin (1) y 3- (1,1´-dimethyl-3´ nitro allyl-herniarin] (3) (NHR) derived from coumarin, which have excellent antidepressant activity. The compound 3- (1,1´-dimethyl-3´ nitro allyl-herniarin] (3) (NHR) is synthesised by means of a nitration reaction of the compound 3-(1´,1´-dimethylallyl)-herniarin. The present invention also relates to the method for the isolation and synthesis of the compound 3 -(1´,1´-dimethylallyl)-herniarin.

专利号:US-2009264680-A1
优先权日:2004-07-07
标题:Process for the synthesis and purification of (4-methoxybutyl) (4-trifluoromethylphenyl) methanone
发明人：CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA
权利人:CASTELLIN ANDREA; GREGORI LUCA; GONZALES TRUEBA GUADALUPE; RUBELLO ALBINO; NICOLE ANDREA
摘要:A process for the preparation of 4-trifluoromethylvalerophenone is described. The process described is a three step process comprising the synthesis of organomagnesium specie, coupling reaction between the organomagnesium specie and trifluoromethylbenzonitrile or trifluoromethylbenzoyl chloride and preferably a purification of the product obtained in suitable reaction conditions. In the process an extraction phase of the final product is not required.

专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.