Reference

Synthesis of irbesartan

Synthesis of irbesartan. Nisnevich, Gennady; Rukhman, Igor; Pertsikov, Boris; Kaftanov, Julia; Dolitzky, Ben-Zion; Shapiro, Eugeny; Yahalomi, Bonit (Teva Pharmaceutical Industries Ltd.; Teva Pharmaceuticals USA, Inc., Israel). PCT Int. Appl. WO 2004007482 A2 22 Jan 2004, 13 pp. DESIGNATED STATES: W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW, AM, AZ, BY, KG, KZ, MD, RU; RW: AT, BE, BF, BJ, CF, CG, CH, CI, CM, CY, DE, DK, ES, FI, FR, GA, GB, GR, IE, IT, LU, MC, ML, MR, NE, NL, PT, SE, SN, TD, TG, TR. (English). (World Intellectual Property Organization). CODEN: PIXXD2. CLASS: ICM: C07D403-00. APPLICATION: WO 2003-US22479 16 Jul 2003. PRIORITY: US 2002-PV396424 16 Jul 2002; US 2002-PV402490 9 Aug 2002. DOCUMENT TYPE: Patent CA Section: 28 (Heterocyclic Compounds (More Than One Hetero Atom)) Irbesartan is prepd. by reaction of 2-butyl-1,3-diaza-spiro[4.4]non-1-ene (I) with 5-(4-bromomethylbiphenyl-2-yl)-1-trityl-1H-tetrazole (II) in the presence of a phase transfer catalyst. 138402-05-8 and 138402-10-5 which are cas registry numbers of substances are two of reagents here. Thus, reaction of I with II in toluene in the presence of Bu4NHSO4 at 90° for 1.5 h gave, after deprotection, 84.3% irbesartan. Also provided is irbesartan having a fine particle size. .