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1. (WO2009059765) PROCESS FOR THE PREPARATION OF DROSPIRENONE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/059765    International Application No.:    PCT/EP2008/009372
Publication Date: 14.05.2009 International Filing Date: 06.11.2008
IPC:
C07J 1/00 (2006.01), C07J 31/00 (2006.01), C07J 53/00 (2006.01), A61K 31/585 (2006.01), A61P 15/18 (2006.01)
Applicants: CHORISIS S.R.L. [IT/IT]; Via Mons. Colombo, 30/32, I-22066 Mariano Comense (CO) (IT) (For All Designated States Except US).
GALLIANI, Guido [IT/IT]; (IT) (For US Only).
RADAELLI, Vincenzo [IT/IT]; (IT) (For US Only).
TERRANEO, Alberto [IT/IT]; (IT) (For US Only)
Inventors: GALLIANI, Guido; (IT).
RADAELLI, Vincenzo; (IT).
TERRANEO, Alberto; (IT)
Agent: MINOJA, Fabrizio; Bianchetti Bracco Minoja S.r.l., Via Plinio, 63, I-20129 Milano (IT)
Priority Data:
MI2007A002141 08.11.2007 IT
Title (EN) PROCESS FOR THE PREPARATION OF DROSPIRENONE
(FR) PROCÉDÉ DE PRÉPARATION DE DROSPIRÉNONE
Abstract: front page image
(EN)The present invention describes a process for the preparation of drospirenone (I) using androstendione as a starting material. In particular, androstendione protected on carbonyl group in position 3 as an enol-ether is functionalized in position 16 with a sulfoxide group and the derivative thus obtained undergoes thermal elimination in alkaline to give androsta-4,15- diene-3, 17-dione (V) which is further transformed into Drospirenone (I).
(FR)La présente invention décrit un procédé pour la préparation de drospirénone (I) à l'aide d'androstènedione comme matière de départ. En particulier, l'androstènedione protégée sur le groupe carbonyle en position 3 sous la forme d'un énol-éther est fonctionnalisée en position 16 par un groupe sulfoxyde et le dérivé ainsi obtenu subit une élimination thermique en milieu alcalin pour donner l'androsta-4,15- diène-3,17-dione (V) qui est par la suite transformée en Drospirénone (I).
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, ST, 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)