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1. (WO2008098527) METHOD FOR THE PREPARATION OF 5-BENZYLOXY-2-(4-BENZYLOXPHENYL)-3-METHYL-1H-INDOLE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2008/098527    International Application No.:    PCT/CZ2008/000016
Publication Date: 21.08.2008 International Filing Date: 11.02.2008
IPC:
C07D 209/12 (2006.01), C07C 217/80 (2006.01)
Applicants: ZENTIVA A.S. [CZ/CZ]; U kabelovny 130, 102 37 Praha 10 (CZ) (For All Designated States Except US).
JIRMAN, Josef [CZ/CZ]; (CZ) (For US Only).
RICHTER, Jindrich [CZ/CZ]; (CZ) (For US Only)
Inventors: JIRMAN, Josef; (CZ).
RICHTER, Jindrich; (CZ)
Agent: JIROTKOVA, Ivana; Rott, Ruzicka & Guttmann, Patent, Trademark & Law Offices, Nad Stolou 12, 170 00 Praha 7 (CZ)
Priority Data:
PV 2007-110 12.02.2007 CZ
Title (EN) METHOD FOR THE PREPARATION OF 5-BENZYLOXY-2-(4-BENZYLOXPHENYL)-3-METHYL-1H-INDOLE
(FR) PROCÉDÉ D'ÉLABORATION DE 5-BENZYLOXY-2-(4-BENZYLOXPHÉNYL)-3-MÉTHYL-1H-INDOLE
Abstract: front page image
(EN)A method for the preparation of 5-benzyloxy-2-(4-benzyloxyphenyl)-3-methyl-1H-indole of formula (1) by reaction of 2-bromo-4'-benzyloxypropiophenone and 4-benzyloxyaniline hydrochloride, in which high purity of the product is achieved by isolation of the intermediate, N-(4-benzyloxyphenyl)-α-amino-4-benzyloxypropiophenone of formula (10), in the solid state. The method may be used for the preparation of bazedoxifen of formula (2).
(FR)procédé d'élaboration de 5-benzyloxy-2-(4-benzyloxphényl)-3-méthyl-1H-indole de formule (1) par réaction entre 2-bromo-4'-benzyloxypropiophénone et hydrochlorure de 4-benzyloxyaniline, sachant que la pureté élevée du produit résulte de l'isolation de l'intermédiaire N-(4-benzyloxyphényl)-α-amino-4-benzyloxypropiophénone de formule (10), à l'état solide. On peut utiliser le procédé pour produire du bazedoxifène de formule (2).
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)