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多拉韦林合成路线图解 被引量:1

Graphical synthetic routes of doravirine
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摘要 多拉韦林(doravirine,MK-1439,1)化学名为3-氯-5-[[1-[(4,5-二氢-4-甲基-5-氧代-1H-1,2,4-三唑-3-基)甲基]-1,2-二氢-2-氧代-4-(三氟甲基)-3-吡啶基]氧基]苯甲腈,CAS登记号为1338225-97-0。该药是默克公司开发的新一代HIV非核苷类逆转录酶抑制剂,对HIV-1野生株和耐药突变株都有较强的抑制活性,其活性优于现有的非核苷类药物。 Doravirine is a novel HIV non-nucleoside reverse transcriptase inhibitor in the phase Ⅲ clinical trial,which possesses the desired properties for further development as new antiviral drug candidate for the treatment of HIV-1 infection.This article summarizes the different synthetic routes of doravirine.
出处 《中国药物化学杂志》 CAS CSCD 2016年第1期74-76,7,共3页 Chinese Journal of Medicinal Chemistry
基金 国家自然科学基金重点国际合作研究项目(81420108027) 国家自然科学基金面上项目(81273354)
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  • 1LAI M T, FENG M, FALGUEYRET J P, et al. In vitro characterization of MK-1439, a novel HIV-1 non-nucleoside reverse transcriptase inhibitor [J]. Antimicrob Agents Chemother ,2014,58 ( 3 ) : 1652 - 1663. 被引量:1
  • 2ANDERSON M S, GILMARTIN J, CILISSEN C, et al. Safety, tolerability and pharmacokinetics of dora- virine, a novel HIV non-nucleoside reverse tran- scriptase inhibitor, after single and multiple doses in healthy subjects [ J ]. Anfivir Ther, 2014, 20 ( 4 ) : 397 - 405. 被引量:1
  • 3BURCH J, COTE B, NGUYEN N, et al. Non-nucleo- side reverse transcriptase inhibitors :2011120133 [ P]. 2011 - 10 - 06. 被引量:1
  • 4ITOH T, JEON I, MANGION I, et al. Process for making reverse transcriptase inhibitors: 2014089140 [P].2014 -06 - 12. 被引量:1
  • 5GAUTHIER D R Jr, SHEERY B D, CAO Y, et al. Highly efficient synthesis of HIV NNRTI doravirine [J]. Org Lett,2015,17(6) :1353 - 1356. 被引量:1
  • 6COTE B, BURCH J D, ASANTE-APPIAH E, et al. Discovery of MK-1439, an oraily bioavailable non- nucleoside reverse transcriptase inhibitor potent against a wide range of resistant mutant HIV viruses [J]. Bioorg Med Chem Lett, 2014,24 ( 3 ) : 917 - 922. 被引量:1
  • 7COWDEN C J,WILSON R D,BISHOP B C,et al. A new synthesis of 1,2,4-tdazolin-5-ones : application to the convergent synthesis of an NK1 antagonist [ J]. Tetrahedron Lett,2000,41 (44) :8661 - 8664. 被引量:1

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