Patent SG-11201406945Q-A (SG)
Title: Process for the preparation of 2-deoxy-2-fluoro-2-methyl-d-ribofuranosyl nucleoside compounds
Inventor: CARR ROBERT
IPC: C07H19/06
Filed: 2013-05-27
Abstract: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 5 December 2013 (05.12.2013) WIPOIPCT (10) International Publication Number WO 2013/178571 A1 (51) International Patent Classification: C07H1/00 (2006.01) A61P 31/12 (2006.01) C07H19/06 (2006.01) (21) International Application Number: (22) International Filing Date: (25) Filing Language: (26) Publication Language: PCT/EP2013/060836 27 May 2013 (27.05.2013) English English (30) Priority Data: 12169760.1 29 May 2012 (29.05.2012) EP (71) Applicant (for all designated States except US): F. HOFF­ MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124, CH-4070 Basel (CH). (71) Applicant (for US only): HOFFMANN-LA ROCHE INC. [US/US]; 340 Kingsland Street, Nutley, New Jersey 07110 (US). (72) Inventors: CARR, Robert; 229 E. Smallwood Road, Eff­ ingham, South Carolina 29541 (US). HILDBRAND, Stefan; Loerenweg 7, CH-4460 Gelterkinden (CH). HODGES, Mark L.; 721 Lindsey Drive, Florence, South Carolina 29501 (US). KAMMERER, Michael; Kornhaus- gasse 2, CH-4051 Basel (CH). LANG, John F.; 900 Cloisters Drive, Florence, South Carolina 29505 (US). LAWRIMORE III, William J.; 2766 Olde Mill Road, Florence, South Carolina 29505 (US). NGUYEN, Dieu; 1 Olson Street #6, Wilmington, Massachusetts 01887 (US). (74) Agent: RAUBER, Beat; Grenzacherstrasse 124, CH-4070 Basel (CH). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, 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, PA, 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. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (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), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv)) Published: — with international search report (Art. 21(3)) (54) Title: PROCESS FOR THE PREPARATION OF 2-DEOXY-2-FLUORO-2-METHYL-D-RIBOFURANOSYL NUCLEOSIDE COMPOUNDS R CO 1 l> oo i> R CO: (I) T-H o CJ (57) Abstract: An improved process for the preparation of (2'R)-2'-deoxy-2'-fluoro-2-methylcytidine derivatives , of formula I, (I), wherein R 1 is selected from Ci-4-alkyl is described. The (2'R)-2'-deoxy-2'-fluoro-2-methylcytidine derivatives , of formula I have the potential to be useful as prodrugs for potent inhibitors of the Hepatitis Virus (HCV) C NS5B polymerase.