[(1S,2R)-1-苄基-2-羟基-3-(异丁基氨基)丙基]氨基甲酸叔丁酯的合成
摘要
以环氧化氨基苯丁烷和异丁胺为起始材料,将反应条件进行优化,最后合成[(1S,2R)-1-苄基-2-羟基-3-(异丁基氨基)丙基]氨基甲酸叔丁酯;其转化率为99%,收率达到92-95%。
出处
《科技视界》
2017年第30期178-178,180,共2页
Science & Technology Vision
二级参考文献23
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1Kilaru RB, Valasani KR, Yellapu S, et al. First stereoselective total synthesis of(3R, 3aS, 6aR)-hexahydrofuro[2,3-b]furan- 3yl(2R,3 S)-4-(4-amino-N-isobutyl phenylsulfonamido)- 3-hydroxy- 1-phenylbutan-2-yl-carbamate(diastereomer of Darunavir)[J]. Indian J Chemistry, 2012, 51:849-854.
-
2Pauwels R. Mini-review: aspects of successful drug discovery and development[J]. Antivir Res, 2006, 71:77-89.
-
3Martinez-Cajas JL, Wainberg MA. Protease inhibitor resistance in HIV infected patients: molecular and clinical perspectives. Antivir [J]. Res, 2007,76: 203-221.
-
4D'Avolio A, Siccardi M, Sciandra M, et al. HPLC-MS method for the simultaneous quantification of the new HIV protease inhibitor darunavir, and 11 other antiretroviral agents in plasma of HIV-infected patients [J]. J Chromatogr, 2007, 859: 234-240.
-
5Ghosh AK, Dawson ZL, Mitsuya H. Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV [J]. Bioorg Med Chem, 2007, 15: 7576-7580.
-
6Kovalevsky AY, Liu F, Leshchenko S, et al. Ultra-high resolution crystal structure of HIV-1 protease mutant reveals two binding sites for clinical inhibitor TMC114 [J]. J Mol Biol, 2006, 363: 161-173.
-
7Yeni P. Update on HAART in HIV [J]. J Hepatol, 2006, 44:100-103.
-
8King NM, Prabu-jeyabalan M, Nalivai KA, et al. Structural and thermdynamic basis for the binding of TMCll4, an ext-generation human immunodeficiency virus typel protease inhibitor[J]. J Viol, 2004, 78(21): 12012-12021.
-
9Michael L. a-and 13-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors[P]. US: 5843946, 1998-12-01.
-
10Michael L, a-and 13-amino acid hydroxyethylamino sulfonamides useful as retroviral protease inhibitors[P]. US: 6248775, 1998-06-19.
共引文献3
-
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-
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-
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-
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-
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