CAS: 174485-72-4; 5-(Trifluoromethyl)Pyridine-2-Sulfonyl Chloride

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1806784-58-6 179400-16-9 1805273-82-8

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CAS号76041-72-0 2-巯基-5-(三氟甲基)吡啶 | CAS号2637-34-5 2-巯基吡啶 | CAS号174484-41-4 替拉那韦 | CAS号1141510-06-6 N-Hydroxy Tipranavir

📜2-巯基-5-(三氟甲基)吡啶置于盐酸,氯体系中,用 水 用作溶剂,化学反应 1.5H,以89%的收率获得5-三氟甲基吡啶-2-磺酰氯
参考文献:Synthesis Of [14C]-And [13C6]-Labeled Tipranavir And Its Potential Hydroxyl Metabolite And The Glucuronide Conjugate
标题:Synthesis Of [14C]-And [13C6]-Labeled Tipranavir And Its Potential Hydroxyl Metabolite And The Glucuronide Conjugate
摘要:替普瑞那韦或 Aptivus® 是一种非肽蛋白酶抑制剂,已被批准与利托那韦联合治疗艾滋病病毒感染.在进行药物代谢(排泄,分布和吸收)研究和开发支持临床研究所需的生物分析方法时,需要使用放射性和稳定碳同位素标记的替普瑞那韦.[7-14C]-苯甲酸和均匀标记的苯甲酸(环-13C6 99 At% 13C)分别用于制备[14C]-和[13C6]-标记的替拉那韦.放射性标记的替拉那韦的比活度为 54 Mci/mmol(2Gbq/mmol);由于其不稳定性,必须用未标记的替拉那韦将其比活度稀释至 28 Mci/mmol(46.45 µci/mg).此外,还合成了替拉那韦最丰富的代谢物 N-羟基代谢物 (12) 和葡萄糖醛酸结合物 (13)(与利托那韦同时服用时).Copyright © 2008 John Wiley & Sons,Ltd. All Rights Reserved.
Doi:10.1002/jlcr.1528

专利信息

专利号:US-2004110957-A1
优先权日:2002-12-05
标 题 :Process for the synthesis of an antiviral compound
发明人：WILKEN JOERG; NERENZ FRANK; KANSCHIK-CONRADSEN ANDREAS
权利人:HONEYWELL INT INC
摘要:In a process comprising synthesizing pyranes including [R—(R*,R*)]-N-[3-[1-[5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide the present invention comprises the improvements comprising: (a) providing a racemic mixture of 3-hydroxy-3-(2-phenylethyl)-hexanoate ethyl acetate by reacting said 1-phenyl-hexan-3-one with ethylbromoacetate under Reformatsky conditions; and (b) separating (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid in enantiomeric excess by saponification and reverse resolution of the racemate of step (a) to produce a resolved product. In addition, the present invention comprises a reverse resolution process for separating an enantiomer from a mixture of enantiomers.

专利号:US-2010184989-A1
优先权日:2007-03-12
标 题 :De Novo Synthesis of Conjugates
发明人：RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J
权利人:NEKTAR THERAPEUTICS
摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.

专利号:AU-2008226820-A1
优先权日:2007-03-12
标题 :De novo synthesis of conjugates

专利号:US-6852711-B2
优先权日:1998-09-11
标题:HIV protease inhibitors
发明人：BOYER JR FREDERICK EARL; DOMAGALA JOHN MICHAEL; ELLSWORTH EDMUND LEE; GAJDA CHRISTOPHER ANDREW; HAGEN SUSAN ELIZABETH; LOVDAHL MICHAEL JAMES; LUNNEY ELIZABETH ANN; MARKOSKI LARRY JAMES; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN
权利人:AGOURON PHARMA
摘要:The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.

专利号:CA-2679473-A1
优先权日:2007-03-12
标题:De novo synthesis of conjugates

专利号:EP-2125027-A2
优先权日:2007-03-12
标题:De novo synthesis of conjugates