CAS: 59729-33-8; Citalopram

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CAS号103146-25-4 4-(4-(二甲基氨基)-1-... | CAS号445312-08-3 3-chloromethyl-... | CAS号19070-16-7 magnesium,N,N-d... | CAS号773837-37-9 sodium cyanide | CAS号64169-45-5 1-(4-氟苯基)-1-(3-... | CAS号64372-56-1 1-[3-(二甲基氨基)丙基]... | CAS号64169-39-7 5-溴去氰基西酞普兰 | CAS号544-92-3 氰化亚铜 | CAS号64169-66-0 5-溴-1-(4-氟苯基)-酞内酯 | CAS号59729-32-7 氢溴酸西酞普兰 | CAS号128196-01-0 艾司西酞普兰 | CAS号128196-02-1 (R)-西酞普兰 | CAS号64372-56-1 1-[3-(二甲基氨基)丙基]...

4-(4-二甲胺基-1-对氟苯基-1-羟基丁基)-3-(羟甲基)苯腈置于甲基磺酰氯,三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,以55%的收率获得产物西酞普兰
参考文献:Structure−activity Relationships For A Novel Series Of Citalopram (1-(3-(Dimethylamino)Propyl)-1-(4-Fluorophenyl)-1,3-Dihydroisobenzofuran-5-Carbonitrile) Analogues At Monoamine Transporters
标题:Structure−activity Relationships For A Novel Series Of Citalopram (1-(3-(Dimethylamino)Propyl)-1-(4-Fluorophenyl)-1,3-Dihydroisobenzofuran-5-Carbonitrile) Analogues At Monoamine Transporters
摘要:(+/−)-Citalopram(1,1-(3-(二甲基氨基)丙基)-1-(4-氟苯基)-1,3-二氢异苯并呋喃-5-腈),及其eutomer(纯对映体),艾司西酞普兰(s-(+)-1)是选择性5-羟色胺再摄取抑制剂(ssris),临床上用于治疗焦虑和抑郁.为了进一步探索5-羟色胺转运体(sert)处的构效关系,设计,合成了(+/-)-4-和5-取代的西酞普兰类似物,并在啮齿类动物的天然组织中评估了它们对sert,多巴胺转运体(dat)和去甲肾上腺素转运体(net)的结合能力.许多这些类似物显示出高sert结合亲和力(k-I = 1-40 Nm),并且对net和dat具有选择性.合成了一些对映体类似物,其中s-和r-对映体在sert处均保持了对映选择性,且s > R.此外,1和5的对映体对在同源的细菌亮氨酸转运体(leut)上的结合能力也被测试,结果显示低亲和力和缺乏对映选择性,这表明这些化合物在sert上的结合位点与leut相比是独特的.这些新型配体将为阐明药物与蛋白质在sert处的相互作用提供分子工具,并将这些作用与体内行为反应相关联.
DOI:10.1021/jm1005034

专利信息

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-2008119662-A1
优先权日:2004-02-16
标 题:One Spot Synthesis of Citalopram from 5-Cyanophthalide
发明人：NARAHARI BABU AMBATI; SRINIVAS GOUD VUDDAMARI; GAONKAR SANTOSH LAXMAN; MANJUNATHA SULUR G; KULKARNI ASHOK KRISHNA; KULKARNI MADHARI A
权利人:JUBILANT ORGANOSYS LIMTED
摘要:A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5-cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.

专利号:US-2006030625-A1
优先权日:2004-08-06
标 题 :Dietary neurotransmitter precursors for balanced synthesis of neurotransmitters
发明人：HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT
权利人:HART CHERYLE RAM; GROSSMAN RONALD S; RAM HERBERT
摘要:Dietary supplements for treating a neurotransmitter deficiency include one or more precursors of the deficient neurotransmitter and a cofactor for activating in vivo enzymatic synthesis of the deficient neurotransmitter. The dietary supplements can also include an appropriate neurotransmitter, such as an amino acid. When administered through the oral mucosa, increases in levels of the deficient neurotransmitters and relief from deficiency symptoms are obtained.

专利号:WO-0102383-A8
优先权日:1999-07-06
标 题:Process for the synthesis of citalopram
发明人：BOLZONELLA EVA; CASTELLIN ANDREA; NICOLE ANDREA
权利人:LUNDBECK PHARMACEUTICALS ITALY; BOLZONELLA EVA; CASTELLIN ANDREA; NICOLE ANDREA
摘要:A new process is described for the synthesis of citalopram characterized by the conversion of 1-(4'-fluorophenyl)1-3-(dimethylaminopropyl)-5-halophthalane in the corresponding Grignard reagent; this intermediate product may be converted into citalopram via intermediate formation of an aldehyde and in the subsequent transformation of the functional group via oxime or hydrazone; or else be converted into citalopram via reaction with compounds containing a cyano group bound to a leaving group. The process described makes it possible to obtain citalopram in high yields, and does not involve the use of drastic conditions of temperature.

专利号:US-9597327-B2
优先权日:2005-05-25
标 题:Synthesis of (R)-N-methylnaltrexone
发明人：DOSHAN HAROLD D; PEREZ JULIO
权利人:PROGENICS PHARM INC
摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.

专利号:US-12234200-B2
优先权日:2019-04-16
标 题:Synthetic methods of preparing esketamine
发明人：CHEN CHENG YI
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.