| abstract |
It refers to 4'-ethynyl-2-fluoro-2'-deoxyadenosine (EFdA) diesters of Formula II, wherein: R1 and R2 are -C(=O)R3 and R3 is isopropyl, 3-pentyl, cyclopentyl, phenyl or phenylmethyl. Among the preferred compounds we have the following: (2R,3S,5R)-5-(6-amino-2-fluoro-9Hpurin-9-yl)-2-(((2-ethylbutanoyl)oxy)methyl 2-ethylbutanoate )-2-ethynyltetrahydrofuran-3-yl; (2R,3S,5R)-5-(6-amino-2-fluoro-9Hpurin-9-yl)-2-ethynyl-2-((2-phenylacetoxy)methyl)tetrahydrofuran-3-yl 2-phenylacetate; among others. These compounds are crystalline and useful in providing extended in vivo viral suppression of human immunodeficiency virus (HIV). |