Detail of "73615-83-5"

Reference

Preparation of pyridinone derivatives as HIV reverse transcriptase inhibitors

Hoffman, Jacob M., Jr.; Rooney, Clarence S.; Saari, Walfred S.; Wai, John S.; Williams, Theresa M.; Bamberger, Dona L.; Jones, James H. (Merck and Co., Inc., USA). Eur. Pat. Appl. EP 462800 A2 27 Dec 1991, 87 pp. DESIGNATED STATES: R: AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LI, LU, NL, SE. (European Patent Organization). CODEN: EPXXDW. CLASS: ICM: C07D213-64. ICS: C07D213-76; C07D401-06; C07D401-12; C07D407-06; C07D407-12; C07D409-06; C07D409-12; C07D413-06; C07D413-12; C07D417-06. ICA: C07D417-12; A61K031-44. APPLICATION: EP 91-305502 18 Jun 1991. PRIORITY: US 90-539643 18 Jun 1990; US 90-539681 18 Jun 1990; US 91-646131 25 Jan 1991; US 91-712217 7 Jun 1991.There are some commonly used reagents with their cas registry numbers 73615-83-5 and 139548-15-5 in this article. DOCUMENT TYPE: Patent CA Section: 27 (Heterocyclic Compounds (One Hetero Atom)) Section cross-reference(s): 1, 28 Title compds. I [X = NR, O, S, CHR, SO, SO2, CO, CHOR, CH2CHOH, CH2CO, RC:CR, NCOR, NCH2CO2R, NRSO, NRSO2, NRCO; R = H, alkyl, alkenyl, C3-8 cycloalkyl; Z = O,S, (C1-8 alkyl)amino; n = 0-4; R1,R2,R4 = H, (substituted) alkyl, C3-8 cycloalkyl, C1-5 alkylthio, alkylsulfinyl, alkylsulfonyl, alkoxy, alkoxycarbonyl, etc.; R1R4 or R1R2 may form 5-7 membered cycloalkyl; R3,R5 = groups defined for R; Y = (substituted) aryl, (substituted) heterocyclyl; Y 1 phthalimidyl; R1 1 R2 = OH] were prepd. as HIV reverse transcriptase inhibitors useful for the treatment of AIDS and ARC. Thus, cyclocondensation of 2-ethyl-3-oxobutanal Na salt with O2NCH2CONH2 gave 5-ethyl-6-methyl-3-nitro-2(1H)-pyridinone, which was hydrogenated to give the 3-amino deriv. N-alkylation of the letter with 2-bromomethylnaphthalene gave title compd. I [R1 = Et; R2 = Me; R3-R5 = H; X = NH; n = 1; Y = 2-naphthyl] I are said to inhibit HIV reverse transcriptase with IC50's of 7-30 nM. .