Reference

Preparation of 4-difluorophenylcarbonyl-1-methylpyrrolidinylpropyloxyphenyl-piperazin- 2-one as H1 receptor activators for treatment of allergic rhinitis

All Rights Reserved. Preparation of 4-difluorophenylcarbonyl-1-methylpyrrolidinylpropyloxyphenyl-piperazin- 2-one as H1 receptor activators for treatment of allergic rhinitis. Ancliff, Rachael Ann; Bamford, Mark James; Hodgson, Simon Teanby; Parr, Christopher Allan; Procopiou, Panayiotis Alexandrou; Wilson, David Matthew; Woodrow, Michael (Glaxo Group Limited, UK). PCT Int. Appl. WO 2007009739 A1 25 Jan 2007, 39pp. 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. (English). (World Intellectual Property Organization). CODEN: PIXXD2. APPLICATION: WO 2006-EP7034 17 Jul 2006. PRIORITY: GB 2005-14811 19 Jul 2005. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Section cross-reference(s): 1, 63 Title compds. I was prepd. by reaction of 1-[4-[[3-(2-methyl-1-pyrrolidinyl)propyl]oxy]phenyl]-2-piperazinone (prepn. given) with 2,4-difluorobenzoic acid, which is useful as H1 receptor activators for treatment of allergic rhinitis. I was tested in Histamine H1 & H3 functional antagonist assay, and showed an av. pKi at H3 of greater than about 8.5 and at H1 of less than about 5.7. In addn., I showed an oral bioavailability of approx. 48%F in rat and of approx. 100%F in dog with a CNS penetration of about 57.5 ng/g.Except for chemicals metioned above, 1583-58-0 is also used. .

NMR Tube Filter Reactor for Solid-Phase Synthesis and Gel-Phase 19F NMR Spectroscopy

NMR Tube Filter Reactor for Solid-Phase Synthesis and Gel-Phase 19F NMR Spectroscopy. Wallner, Fredrik K.; Elofsson, Mikael (Organic Chemistry Department of Chemistry, Ume University, Ume SE-90187, Swed.). 1583-58-0 which is the cas registry number of some chemical is mentioned. Journal of Combinatorial Chemistry, 8(2), 150-152 (English) 2006 American Chemical Society. CODEN: JCCHFF. ISSN: 1520-4766. DOCUMENT TYPE: Journal CA Section: 34 (Amino Acids, Peptides, and Proteins) Section cross-reference(s): 22 To facilitate gel-phase NMR spectroscopy, the authors designed a modified NMR tube that is suitable for solid-phase peptide synthesis. Using this reactor and TentaGel resin, peptide L-N-(2,4-difluorobenzoyl)-4-fluorophenylalanylglycine was synthesized and analyzed by 19F NMR spectroscopy. 1583-58-0 is just another one chemical used in this study. ..