CAS: 106133-20-4; (R)-5-(2-((2-(2-Ethoxyphenoxy)Ethyl)Amino)Propyl)-2-Methoxybenzenesulfonamide

上下游产品

2-(2-ethoxyphenoxy)acetaldehyde (S)-5-(2-hydroxypropyl)-2-methoxybenzenesulfonamide (R)-5-(2-azidopropyl)-2-methoxybenzenesulfonamide (S)-1-(4-methoxy-3-sulfamoylphenyl)propan-2-yl acetatetamsulosin hydr°Chloride (R)-tamsar°Cin (-)-camphor-10-sulfonate tamsulosin hydr°Chloride (R)-tamsulosin(+)-tartrate salt

5-((R)-2-((2-(2-Ethoxy)Phenoxyethyl)((R)-1-Phenylethyl)Amino)Propyl)-2-Methoxybenzenesulfonamide置于甲醇,Palladium 10% On Activated Carbon,甲酸铵体系中,用76.5%的收率获得坦索洛新
参考文献:一种盐酸坦索罗辛的制备方法
标题:一种盐酸坦索罗辛的制备方法
摘要:本发明属于化学合成技术领域,涉及一种盐酸坦索罗辛的合成方法.该合成方法将如式(II)所示的苯磺酰胺先与式(III)所示的溴醚反应得到如式(iv)所示的缩合物中间体,中间体式(iv)在甲酸铵及催化剂的存在下,转移氢化反应后,得到如式(v)所示的r‑坦索罗辛游离碱,该r‑坦索罗辛游离碱在有机溶剂中与盐酸进行成盐反应,得到如式(i)所示的盐酸坦索罗辛.其特征在于,其中式(II)与式(III)反应是在含有水的溶剂中进行的.通过本发明的合成路线,得到的盐酸坦索罗辛的反应过程中不存在两分子的溴化物与胺反应生成二取代副产物,获得的盐酸坦索罗辛具有产品纯度好,质量稳定,收率高,本发明的反应条件温和,合成方便.

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-8193384-B2
优先权日:2005-07-29
标 题 :Polymer-bound phosphitylating reagents for the synthesis of organophosphorus compounds
发明人：PARANG KEYKAVOUS; AHAMDIBENI YOUSEF
权利人:PARANG KEYKAVOUS; AHAMDIBENI YOUSEF; RHODE ISLAND EDUCATION
摘要:The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.

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:WO-2012101648-A1
优先权日:2011-01-24
标题:Novel process for the synthesis of enantiomerically pure 2-methoxy-5-[(2r)-2-(4-alkylpiperazin-l-yl)propyl]-benzenesulfonamide
发明人：HAVALDAR FREDDY H; DABHOLKAR BHUSHAN VASANT; MULE GANESH BABAN
权利人:HAVALDAR FREDDY H
摘要:Where R is C1-C3 alkyl, alkenyl A novel process for synthesis of compound of Formula 1 comprising steroselective catalytic reduction of compound of Formula IV under hydrogen gas pressure to obtain an intermediate compound of Formula II, which on coupling in presence of coupling agent and base in presence of organic solvent to obtain compound of Formula X, Formula X on reacting with deprotecting agent in presence of organic solvent results in formation of compound of Formula XI, condensation of Formula XI with alkyl halide results in formation of compound of Formula I.

专利号:US-7619116-B2
优先权日:2003-12-17
标 题:Intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts and process for their preparation
发明人：DAMBRIN VALERY; LENOIR JEAN-YVES; SCHNEIDER JEAN-MARIE; GUILLAMOT GERARD; FOLLET MICHEL; BECKER ABRAM
权利人:PRODUCTS CHIMIQUES AUXILIAIRES
摘要:A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.

专利号:US-7538246-B2
优先权日:2003-12-29
标 题:Synthesis of optically pure(r)-5-(2-amynopropyl)-2-methoxybenzenesulphonamide
发明人：MOHAR BARBARA
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to a new process for the preparation of optically pure(R)-5-(2-aminopropyl)-2-methoxybenzenesulphonamide, which is an intermediate in the synthesis of tamsulosin.