On July 31, 2003, Egbertson, Melissa; Melamed, Jeffrey Y.; Langford, H. Marie; Young, Steven D. published a patent.Application In Synthesis of 1-(Bromomethyl)-4-fluoro-2-iodobenzene The title of the patent was Preparation of hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors. And the patent contained the following:
Hydroxynaphthyridinone carboxamides (shown as I; variables defined below; e.g. N-(4-fluorobenzyl)-4-hydroxy-2-oxo-1,2-dihydro-1,5-naphthyridine-3-carboxamide) are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds were employed against HIV infection and AIDS as compounds per se or as pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions (one example given), optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are also described. Although the methods of preparation are not claimed, 27 example preparations of I are included; all have IC50’s <0.5 渭M in a HIV integrase assay and all have IC95's <5 渭M in an assay for inhibition of HIV replication. For I: L = linker connecting the C atom of the Ph ring to the N of the -NH- moiety = single bond, -(C1-6 alkyl)- (un)substituted with -C(O)N(RaRb), -(C0-3 alkyl)-C:C-(C1-3-alkyl)-, -(C0-3 alkyl)-C顚咰-(C1-3-alkyl)-, or -(C0-6 alkyl)-(C3-6 cycloalkyl)-(C0-6-alkyl)-. R1a, R1b, and R1c = H, halogen, -C1-6 alkyl, or -C1-6 haloalkyl; R2a and R2b = H, -C1-6 (un)substituted alkyl, -O-C1-6 (un)substituted alkyl, -OH, halo, -NO2, -CN, -C(O)Ra, -CO2Ra, -S(O)nRa, -SO2N(RaRb), -N(RaRb), -C(O)N(RaRb), -N(Ra)SO2Rb, -OC(O)N(RaRb), -N(Ra)C(O)N(RaRb), -N(Ra)-C1-6-alkyl-C(O)N(RaRb), -N(Ra)-C(O)-C1-6 alkyl-N(RaRb), -N(Ra)C(O)-C(O)N(RaRb), -OCO2Ra, -N(Ra)-SO2N(RaRb), -N(Ra)-SO2-C1-6 alkyl-N(RaRb), -N(Ra)C(O)Rb, -N(Ra)CO2Rb, -S-C1-6 alkyl-C(O)N(RaRb),or -N(SO2Ra)-C1-6 alkyl-C(O)N(RaRb). R3 = H, -C1-6-(un)substituted alkyl, -S(O)nRa, -SO2N(RaRb), -C2-6 (un)substituted alkenyl, -C2-5 (un)substituted alkynyl, -Rk, -S(O)n-C1-6 alkyl-Rk, -N(Ra)C(O)-Rk, or -N(Ra)C(O)-C1-6 alkyl-Rk; each of R4 and R5 = H, -C1-6 (un)substituted alkyl, -SO2N(RaRb), or -C1-6 alkyl-Rm; each Ra and Rb = H, -C1-6 alkyl, or -C3-8 cycloalkyl; Rk is a carbocycle or a heterocycle; each Rm = a carbocycle or a heterocycle; each n = 0, 1 or 2; addnl. details including provisos are given in the claims. The experimental process involved the reaction of 1-(Bromomethyl)-4-fluoro-2-iodobenzene(cas: 70931-59-8).Application In Synthesis of 1-(Bromomethyl)-4-fluoro-2-iodobenzene
The Article related to hydroxynaphthyridinone carboxamide preparation hiv integrase inhibitor, aids drug hydroxynaphthyridinone carboxamide preparation hiv integrase 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 In Synthesis of 1-(Bromomethyl)-4-fluoro-2-iodobenzene
Referemce:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com