CAS: 171049-14-2; Lotrafiban

该化合物是一种化学化合物,被归类为对甘蓝蛋白IIb/IIIa受体具有强力和选择性的对抗者,在血盘组装中起着关键作用,主要调查该物质在预防血栓事件方面的潜在用途,特别是在心血管疾病患者中,该物质的特点在于它能够抑制小盘的活化和集聚,从而减少凝块形成的危险.Lotrafiban通常在临床环境中进行施用,并研究其在各种心血管条件下,包括急性冠状综合症中的效力.其药用植物动力特性包括相对较短的半衰期,需要谨慎地施用疗程来保持治疗水平.此外,Lotrafiban的安全特征在临床试验中得到了评估,突出出血综合症等潜在副作用,如与抗甲状腺疗法常见的出血综合症.

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    (S)-(-)-7-[1-[1'-(T-Butoxycarbonyl)-4,4'-Bipiperidinyl]-Carbonyl]-2,3,4,5-Tetrahydro-4-Methyl-3-Oxo-1H-1,4-Benzodiazepine-2-Acetic Acid 174222-33-4
    (S)-1'-(3-Methoxycarbonylmethyl-4-Methyl-3-Oxo-2,3,4,5-Tetrahydro-1H-Benzo[e][1,4]Diazepone-7-Carbonyl)-[4,4']Bipiperidinyl-1-Carboxylic Acid Tert-Butyl Ester 171049-97-1
    (2S)-2,3,4,5-Tetrahydro-4-Methyl-3-Oxo-7-[[4-(4-Pyridinyl)-1-Piperidinyl]Carbonyl]-1H-1,4-Benzodiazepine-2-Acetic Acid 363138-98-1
    (2S)-2-(Carbomethoxymethyl)-4-Methyl-3-Oxo-2,3,4,5-Tetrahydro-1H-1,4-Benzodiazepine-7-Carboxylic Acid 171050-05-8
    2-[(2S)-4-Methyl-7-[(2-Methylpropan-2-yl)Oxycarbonyl]-3-Oxo-2,5-Dihydro-1H-1,4-Benzodiazepin-2-Yl]Acetic Acid 210288-65-6
    (S)-2-Methoxycarbonylmethyl-4-Methyl-3-Exo-2,3,4,5-Tetrahydro-1H-Benzo-[e][1,4]Diazepine-7-Carboxylic Acid Tert-Butyl Ester 171050-04-7
    (4-Methyl-3-Oxo-2,3,4-Tetrahydro-1H-Benzo[e][1,4]Diazepin-2-yl)-Acetic Acid Methyl Ester 193077-87-1
    (7-碘-4-甲基-3-氧代-2,3,4,5-四氢-1H-1,4-苯并二氮杂卓-2-基)乙酸 (2S)-2,3,4,5-Tetrahydro-7-Iodo-4-Methyl-3-Oxo-1H-1,4-Benzodiazepine-2-Acetic Acid 210288-67-8 Methyl (2Rs)-7-Bromo-2,3,4,5-Tetrahydro-4-Methyl-3-Oxo-1H-1,4-Benzodiazepine-2-Acetate

    合成工艺路线路线简述

      📜N-Boc-4,4-联哌啶置于盐酸,Sodium Hydroxide,1-(3-二甲基氨基丙基)-3-乙基碳二亚胺,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环,甲醇,氯仿,N,N-二甲基甲酰胺 用作溶剂,化学反应生成洛曲非班
      参考文献:对映体合成sb 214857(一种有效的口服活性非肽纤维蛋白原受体拮抗剂)
      标题:对映体合成sb 214857(一种有效的口服活性非肽纤维蛋白原受体拮抗剂)
      摘要:据报道,Sb 214857的对映体特异性合成是一种有效的非重复性纤维蛋白原受体拮抗剂.合成途径采用分子内芳基氟化物置换形成1,4-苯并二氮杂system系统的七元环作为关键步骤.
      Doi:10.1016/0040-4039(95)02054-3

      海关参考信息

      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-2015158809-A9
      优先权日:2013-02-26
      标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
      发明人：WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
      权利人:XENOPORT INC
      摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

      专利号:US-2005222431-A1
      优先权日:2003-12-30
      标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

      专利号:US-7227028-B2
      优先权日:2003-12-30
      标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

      专利号:US-2007244331-A1
      优先权日:2003-12-30
      标 题 :Synthesis of Acyloxyalkyl Carbamate Prodrugs and Intermediates Thereof

      专利号:US-2007037988-A9
      优先权日:2003-12-30
      标题 :Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof

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      主要参考文献


      1: Topol EJ, Easton D, Harrington RA, Amarenco P, Califf RM, Graffagnino C, Davis S, Diener HC, Ferguson J, Fitzgerald D, Granett J, Shuaib A, Koudstaal PJ, Theroux P, Van de Werf F, Sigmon K, Pieper K, Vallee M, Willerson JT; Blockade of the Glycoprotein IIb/IIIa Receptor to Avoid Vascular Occlusion Trial Investigators. Randomized, double-blind, placebo-controlled, international trial of the oral IIb/IIIa antagonist lotrafiban in coronary and cerebrovascular disease. Circulation. 2003 Jul 29;108(4):399-406. Epub 2003 Jul 21. Review. doi: 10.1182/blood-2010-03-275990. Epub 2010 May 10. doi: 10.1111/j.1538-7836.2009.03719.x. Epub 2009 Dec 11. Erratum in: J Thromb Haemost. 2010 Nov;8(11):2588.
      14: Salam AM. Is there a role for oral blockade of platelet glycoprotein IIb/IIIa receptors in coronary and cerebrovascular disease? Expert Opin Investig Drugs. 2003 Oct;12(10):1709-12. Review.

      合成参考文献


      摘要:Beccalli, E. M.; Bonetti, A.; Mazza, A., Science of Synthesis: Metal-Catalyzed Cyclization Reactions, (2016) 1, 454.
      参考文献:10.1007/s00018-002-8440-8
      摘要:Casserly IP, Topol EJ. Glycoprotein IIb/IIIa antagonists - from bench to practice. Cellular and Molecular Life Sciences (CMLS). 2002 Mar 01;59(3):478–500. doi: 10.1007/s00018-002-8440-8.
      参考文献:10.2165/00126839-199901050-00002
      摘要:Coleman SG, Duff R. Gp IIb/IIIa antagonists. Summary and table. Drugs R D. 1999 May;1(5):371–3. doi: 10.2165/00126839-199901050-00002.
      参考文献:10.2165/00129784-200101060-00002
      摘要:Chew DP, Bhatt DL, Topol EJ. Oral glycoprotein IIb/IIIa inhibitors: why don't they work Am J Cardiovasc Drugs. 2001;1(6):421–8. doi: 10.2165/00129784-200101060-00002.
      参考文献:10.1134/s1068162008020015
      摘要:Zakutskiĭ AN, Chalisova NI, Subbotina TF. [Functional arginine-containing amino acid sequences in peptides and proteins]. Bioorg Khim. 2008 Mar;34(2):149–59. doi: 10.1134/s1068162008020015.
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