Detail of "574-98-1"

Reference

Preparation of piperidine derivatives as NMDA receptor antagonists

Masui, Moriyasu; Matsumura, Akira (Shionogi & Co., Ltd., Japan). PCT Int. Appl. WO 2006137465 A1 28 Dec 2006, 111pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IS, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (Japanese). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-JP312466 22 Jun 2006. PRIORITY: JP 2005-185100 24 Jun 2005; JP 2005-309760 25 Oct 2005. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1 Title compds. I [A1 = nitrogenated arom. monocyclic group or nitrogenated arom. fused-ring group which has at least one (un)protected hydroxy and/or amino and which may be substituted by other group, nitrogenated arom. monocyclic group or nitrogenated arom. fused-ring group which has -NH- in the ring and in which other ring-constituting atom may have substituent(s) (except (un)protected hydroxy and amino); A2 = (un)substituted arom. cyclic hydrocarbon, (un)substituted arom. heterocycle; R1 = H, hydroxy, acyloxy, etc.; R2 = H, hydroxy, alkyl; R1 and R2 may combine to form single bond; m = 0, 1; X = (un)substituted alkenylene, (un)substituted alkynylene, -CO(CR3R4)n-, etc.; R3, R4 = H, (un)substituted alkyl; n = 0-4; when m is 0, Y represents single bond, -O-, -S-, etc.; when m is 1, Y represents single bond, alkylene, alkenylene, etc.], pharmaceutically acceptable salts or solvates thereof were prepd. For example, EDCI mediated amidation of 4-imidazolecarboxylic acid with compd. II, e. 917755-28-3 and 574-98-1 which are cas registry numbers of chemicals are mentioned.g., prepd. from 4-(4-chlorophenyl)-1,2,3,6-tetrahydropyridine hydrochloride in 2 steps, afforded compd. III [R = imidazol-4-yl] in 35% yield. In NMDA receptor (NR1/NR2B receptor) binding assays, the IC50 value of compd. III [R = 2,3-dihydro-2-oxo-1H-benzimidazol-5-yl] was 0.002 mM. Compds. I are claimed useful as analgesics. .

A mutagenic metabolite synthesized by Salmonella typhimurium grown in the presence of azide is azidoalanine

A mutagenic metabolite synthesized by Salmonella typhimurium grown in the presence of azide is azidoalanine. Owais, W. M.; Rosichan, J. L.; Ronald, R. C.; Kleinhofs, A.; Nilan, R. A. (Dep. Agron. Soils, Washington State Univ., Pullman, WA 99164-6420, USA). Mutat. Res., 118(4), 229-39 (English) 1983. CODEN: MUREAV. ISSN: 0027-5107. DOCUMENT TYPE: Journal CA Section: 4 (Toxicology) A mutagenic azide metabolite was purified from the medium in which S. typhimurium cells were grown in the presence of azide. This metabolite was identified as 3-azidoalanine (I) based on IR and mass spectroscopy and elemental anal. I appeared to be identical to the mutagenic compd. synthesized in vitro from azide and O-acetylserine by partially purified O-acetylserine sulfhydrylase. I mutagenic efficiency and spectrum in S. typhimurium was similar to that of inorg. azide. 2-Azidoethylamine, 2-bromoethylamine, 3-bromopropionic acid, and N-(azidomethyl)phthalimide (II) were also mutagenic with a similar spectrum to azide and I, but with lower efficiency. 3-Azidopropylamine, 4-azidobutylamine, 3-chloroalanine, and ethylamine were only weakly or nonmutagenic. Numerous other chloro, bromo, and azido phthalimide derivs. tested were nonmutagenic. 88192-20-5 and 574-98-1 are just another two chemicals used in this study. Thus, the lack of azide mutagenicity (and perhaps carcinogenicity) in mammalian cells may be due to their inability to convert azide to I. .