WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2012098044) PROCESS FOR THE PREPARATION OF N,N-DIISOPROPYL-3-(2-HYDROXY-5-METHYLPHENYL)- 3-PHENYL PROPYLAMINE AND ITS SALTS STARTING FROM A NOVEL INTERMEDIATE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/098044    International Application No.:    PCT/EP2012/050436
Publication Date: 26.07.2012 International Filing Date: 12.01.2012
IPC:
C07C 213/02 (2006.01), C07C 231/12 (2006.01), C07C 235/34 (2006.01), C07C 215/54 (2006.01)
Applicants: CAMBREX PROFARMACO MILANO S.R.L. [IT/IT]; Via Cucchiari, 17 I-20155 Milano (IT) (For All Designated States Except US).
GIANOLLI, Edoardo [IT/IT]; (IT) (For US Only).
GIANNINI, Elios [IT/IT]; (IT) (For US Only).
BIGINI, Laura [IT/IT]; (IT) (For US Only).
PICCOLO, Oreste [IT/IT]; (IT) (For US Only).
HOLMBERG, Pär [SE/IT]; (IT) (For US Only).
LUNDHOLM, Tommy [IT/IT]; (IT) (For US Only)
Inventors: GIANOLLI, Edoardo; (IT).
GIANNINI, Elios; (IT).
BIGINI, Laura; (IT).
PICCOLO, Oreste; (IT).
HOLMBERG, Pär; (IT).
LUNDHOLM, Tommy; (IT)
Agent: MINOJA, Fabrizio; Bianchetti Bracco Minoja S.R.L. Via Plinio, 63 I-20129 Milano (IT)
Priority Data:
11151066.5 17.01.2011 EP
MI2011A000410 15.03.2011 IT
Title (EN) PROCESS FOR THE PREPARATION OF N,N-DIISOPROPYL-3-(2-HYDROXY-5-METHYLPHENYL)- 3-PHENYL PROPYLAMINE AND ITS SALTS STARTING FROM A NOVEL INTERMEDIATE
(FR) PROCÉDÉ POUR LA PRÉPARATION DE N,N-DIISOPROPYL-3-(2-HYDROXY-5-MÉTHYLPHÉNYL)-3-PHÉNYLPROPYLAMINE ET DE SES SELS À PARTIR D'UN NOUVEL INTERMÉDIAIRE
Abstract: front page image
(EN)The invention concerns an improved process for the preparation of tolterodine (N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenyl propyl amine) and its salts, in particular for the preparation of the tartrate salt, and more particularly for the (+)-(R) enantiomer of tolterodine L-tartrate, starting from a novel intermediate, N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3- phenyl-2-propenamide, which can be used as pure Z or E isomer or as a mixture of Z and E isomers. When the target is the preparation of the enantiomer (R)-(+)-(N,N- diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropylamine) and diastereomeric crystallization of suitable compound is applied, the present invention covers also the use of racemisation of undesired (S)-(-)- (N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3 -phenyl propylamine) enantiomer and its recycle in the process.
(FR)L'invention porte sur un procédé perfectionné pour a préparation de toltérodine (N,N-diisopropyl-3-(2-hydroxy-5-méthylphényl)-3-phénylpropylamine) et de ses sels, en particulier pour la préparation du sel de type tartrate, et plus particulièrement pour l'énantiomère (+)-(R) du L-tartrate de toltérodine, à partir d'un nouvel intermédiaire, le N,N-diisopropyl-3-(2-hydroxy-5-méthylphenyl)-3-phényl-2-propénamide, qui peut être utilisé sous forme de l'isomère Z ou E pur ou sous forme d'un mélange des isomères Z et E. Lorsque l'objectif est la préparation de l'énantiomère (R)-(+)-(N,N-diisopropyl-3-(2-hydroxy-5-méthylphényl)-3-phénylpropylamine) et lorsqu'une cristallisation des diastéréoisomères du composé approprié est appliquée, la présente invention porte également sur l'utilisation de la racémisation de l'énantiomère (S)-(-N,N-diisopropyl-3-(2-hydroxy-5-méthylphényl)-3-phénylpropylamine) non voulu et son recyclage dans le procédé.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, 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, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, 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)