STRUCTURE MODIFICATION OF RITONAVIR WITH CARBAZOLE; SYNTHESIS AND CHARACTERIZATION

被引:0
|
作者
Rao, V. Pandu Ranga [1 ,2 ]
Kumar, N. Senthil [1 ]
Reddy, Shankar B. [1 ]
Islam, Aminul [1 ]
Babu, B. Hari [2 ]
机构
[1] Aurobindo Pharma Ltd, APL Res Ctr 2, Chem Res & Dev, Medak 502329, Andhra Pradesh, India
[2] Acharya Nagarjuna Univ, Dept Chem, Guntur, Andhra Pradesh, India
关键词
Amino acid; Carbazole; HIV-1 protease inhibitors; Ritonavir;
D O I
10.13040/IJPSR.0975-8232.4(9).3601-07
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The core moiety of ritonavir (2S, 3S, 5S)-5-(tert-butyloxycarbonyl) amino-2-amino-3-hydroxy-1,6-diphenylhexane (7) on condensation with oxirane of carbazole (8) in isopropyl alcohol at reflux and deprotected with mineral acid gave compound 10. Coupling of compound 10 with carbamate amino acid (11a-15c) in the presence of EDAC. HCl and HOBt at room temperature gave ritonavir analogues containing carbazole (16a-20c) as a novel for the human immunodeficiency virus (HIV)-1. These compound were characterized by IR, H-1 NMR and Mass spectroscopic.
引用
收藏
页码:3601 / 3607
页数:7
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