1173989-77-9Relevant 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.
experimental part, 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.
