On September 25, 2003, Egbertson, Melissa; Langford, H. Marie; Melamed, Jeffrey Y.; Wai, John S.; Han, Wei; Perlow, Debbie S.; Zhuang, Linghang; Embrey, Mark; Young, Steven D. published a patent.Application of 70931-59-8 The title of the patent was Preparation of N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7-carboxamides useful as HIV integrase inhibitors for treatment of HIV infection/AIDS. And the patent contained the following:
Title compounds I [wherein R1 = H or F; R2 = carbamoylalkyl, carbamoyl, triazolyl or tetrazolyl, acylamino and derivatives, 2-oxopyrrolidin-1-yl and analogs, (cyclo)alkoxycarbonyl, COY; Y = azetidinyl, pyrrolidinyl, piperidinyl, morpholino; R3 = H, carbamoyl and derivatives, acylamino, carbamoyl(alkyl/methylthioxy/methyloxy/amino/alkylamino/alkenyl), (un)substituted 5- to 7-membered saturated heterocyclic ring containing 1 to 4 heteroatoms (N, O or S), (un)substituted 7- to 9-bridged azabicycloalkyl saturated ring; or their pharmaceutically acceptable salts] were prepared as HIV-integrase inhibitors for preventing and treating infection by HIV and for preventing, treating or delaying the onset of AIDS. For example, II鈥a was prepared via TEA-acylation of III鈥Cl (preparation given) with 5-(1,1-dioxo-1,2-thiazinan-2-yl)-8-hydroxy-1,6-naphthyridine-7-carboxylic acid (IV) in DMF at room temperature overnight, followed by sodium salt formation by reaction with NaOH at room temperature for 30 min. IV was prepared from 8-hydroxy-1,6-naphthyridine-7-carboxylic acid Me ester in 5 steps by NBS-bromination in CHCl3, O-tosylation in CHCl3, condensation of the bromide with 1,4-butanesultam in DMF in the presence of Cu2O/2,2′-bipyridyl at 120掳 for 4 h, deprotection of tosyl group, and base-catalyzed hydrolysis in MeOH overnight at 60掳. Selected invention compounds inhibited the strand transfer activity of HIV integrase with IC50 < 0.5 渭M. The same compounds inhibited HIV replication in T-lymphoid cells with IC95 < 5 渭M. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Application of 70931-59-8
The Article related to naphthyridinecarboxamide hiv integrase inhibitor aids composition antiviral, carboxamide naphthyridine hiv replication inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Fused-Ring Systems With Two Or More Hetero Atoms, No More Than One Hetero Atom Per Ring and other aspects.Application of 70931-59-8
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com