【药物名称】L-870810
化学结构式(Chemical Structure):
参考文献No.55144
标题:Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
作者:Young, S.D.; Guare, J.P.; Wai, J.S.; Fisher, T.E.; Perlow, D.S.; Anthony, N.J.; Egbertson, M.; Gomez, R.P.; Kuo, M.S.; Tran, L.; Zhuang, L.; Langford, H.M.; Melamed, J.Y.; Bennett, J.J.; Embrey, M.; Jolly, S.M.; Funk, T.W. (Merck & Co., Inc.)
来源:WO 0230930; WO 0230931
合成路线图解说明:

Mitsunobu coupling between isopropyl 3-(hydroxymethyl)pyridine-2-carboxylate (I) and N-tosyl glycine methyl ester (II) affords amino diester (III). Diester (III) is subsequently converted to the naphthyridine (IV) under Dieckmann cyclization conditions. Bromination of naphthyridine (IV) by means of N-bromosuccinimide provides (V). The methyl ester group of (V) is then displaced with 4-fluorobenzylamine (VI) to furnish amide (VII). Finally, copper-catalyzed displacement of the bromide (VII) with butanesultam (VIII) provides the title compound.

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