1072250-03-3Relevant academic research and scientific papers
Development of practical syntheses of potent non-nucleoside reverse transcriptase inhibitors
Kuethe, Jeffrey T.,Zhong, Yong-Li,Alam, Mahbub,Alorati, Anthony D.,Beutner, Gregory L.,Cai, Dongwei,Fleitz, Fred J.,Gibb, Andrew D.,Kassim, Amude,Linn, Kathleen,Mancheno, Danny,Marcune, Benjamin,Pye, Philip J.,Scott, Jeremy P.,Tellers, David M.,Xiang, Bangping,Yasuda, Nobuyoshi,Yin, Jingjun,Davies, Ian W.
scheme or table, p. 5013 - 5023 (2009/11/30)
The development of practical and efficient syntheses of the potent non-nucleoside reverse transcriptase inhibitors 1 and 2 is described. The preparation of 1 proceeded in four synthetic steps and in 48% overall yield from 3. The long-term synthesis of 2 proceeded in nine synthetic steps and in 47% overall yield from commercially available 2,6-diflurorpyridine. The route to 2 was highlighted by the three-step synthesis of intermediate 22 and the high yielding coupling between 18 and phenol 8. The overall sequence required no chromatography and has successfully been utilized for the manufacture of 2 on large scale.
HIV reverse transcriptase inhibitors
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Page/Page column 53, (2010/11/25)
Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
