On November 3, 2005, Dress, Klaus Ruprecht; Hu, Qiyue; Johnson, Ted William; Plewe, Michael Bruno; Tanis, Steven Paul; Wang, Hai; Yang, Anle; Yin, Chunfeng; Zhang, Junhu published a patent.Category: pyridine-derivatives The title of the patent was Preparation of N-hydroxy pyrrolopyrimidinecarboxamides as inhibitors of HIV integrase.. And the patent contained the following:
Title compounds [I; R1 = H, (substituted) alkyl, alkenyl, heteroalkyl; R2, R5 = H; R3 = (CR8R9)tNR10R11, (substituted) heteroalkyl; R4 = H, halo, alkyl, heteroalkyl, (substituted) alkenyl, alkynyl, OR12a, NR12aR12b; R6 = H, alkyl, heteroalkyl, (substituted) alkenyl; R8, R9 = H, alkyl; R10R11N = (substituted) cycloheteroalkyl; R12a, R12b, R12c = H, alkyl; t = 1-3], were prepared Thus, 1-(2,4-difluorobenzyl)-1H-pyrrolo[2,3-c]pyridine-5-carboxylic acid (preparation given) was stirred with O-(7-azabenzotriazol-1-yl)-1,1,3,3-tetramethyluronium hexafluorophosphate, Et3N, and NH2OH.HCl in DMF for 16 h to give 48% N-hydroxy-1-(2,4-difluorobenzyl)-1H-pyrrolo[2,3-c]pyridine-5-carboxamide. The latter showed an EC50 = 0.00795 μM in an HIV-1 cell protection assay. The experimental process involved the reaction of Methyl 5-amino-4-methylpicolinate(cas: 868551-99-9).Category: pyridine-derivatives
The Article related to pyrrolopyrimidinecarboxamide hydroxy preparation hiv integrase inhibitor, aids arc treatment hydroxamide pyrrolopyrimidine preparation, 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.Category: pyridine-derivatives