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1. (WO2009137337) STEREOSELECTIVE SYNTHESIS OF 17-α -AND 17-β -ARYL STEROIDAL COMPOUNDS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/137337    International Application No.:    PCT/US2009/042404
Publication Date: 12.11.2009 International Filing Date: 30.04.2009
IPC:
C07J 1/00 (2006.01)
Applicants: THE SCRIPPS RESEARCH INSTITUTE [US/US]; 10550 North Torrey Pines Road La Jolla, CA 92037 (US) (For All Designated States Except US).
SHI, Jun [CN/US]; (US) (For US Only).
SHIGEHISA, Hiroki [JP/US]; (US) (For US Only).
GUERRERO, Carlos, A. [US/US]; (US) (For US Only).
SHENVI, Ryan, A. [US/US]; (US) (For US Only).
BARAN, Phil, S. [US/US]; (US) (For US Only)
Inventors: SHI, Jun; (US).
SHIGEHISA, Hiroki; (US).
GUERRERO, Carlos, A.; (US).
SHENVI, Ryan, A.; (US).
BARAN, Phil, S.; (US)
Agent: GAMSON, Edward, P.; Husch Blackwell Sanders Welsh & Katz 120 South Riverside Plaza 22nd Floor Chicago, IL 60606 (US)
Priority Data:
61/050,434 05.05.2008 US
Title (EN) STEREOSELECTIVE SYNTHESIS OF 17-α -AND 17-β -ARYL STEROIDAL COMPOUNDS
(FR) SYNTHÈSE STÉRÉOSÉLECTIVE DE COMPOSÉS STÉROÏDES 17-Α -ET 17-Β -ARYLE
Abstract: front page image
(EN)A process for forming one or the other of a 17-α-aryl or 17-β-aryl steroidal compound in diastereo excess is disclosed. The process utilizes a 17-keto steroid to form a Δ16-17-aryl-steroid compound or a 17-β-hydroxy-17-α-aryl steroid compound that are reduced or deoxygenated, respectively, in the presence of Raney nickel to form a 17-β-aryl- steroid or 17-α-aryl steroid, respectively, in a diastereo ratio of at least 3:1.
(FR)L’invention concerne un processus pour la formation de l’un ou de l’autre d’un composé stéroïde 17-α-aryle ou 17-β-aryle en excès diastéréo-isomérique. Le processus utilise un 17-cétostéroïde pour constituer un composé Δ16-17-aryle stéroïde ou un composé 17-β-hydroxy-17-α-aryle stéroïde qui est réduit ou désoxygéné, respectivement, en présence de nickel de Raney, pour constituer un 17-β-aryle- stéroïde ou un 17-α-aryle stéroïde, respectivement, dans un rapport diastéréo-isomérique d’au moins 3:1.
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, MK, 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)