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1. (WO2010077623) INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF FLUOROGLYCOSIDE DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/077623 International Application No.: PCT/US2009/067079
Publication Date: 08.07.2010 International Filing Date: 08.12.2009
IPC:
C07D 231/20 (2006.01) ,C07H 5/02 (2006.01) ,C07H 13/08 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
14
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
18
One oxygen or sulfur atom
20
One oxygen atom attached in position 3 or 5
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
5
Compounds containing saccharide radicals in which the hetero bonds to oxygen have been replaced by the same number of hetero bonds to halogen, nitrogen, sulfur, selenium, or tellurium
02
to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
H
SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
13
Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
02
by carboxylic acids
08
having the esterifying carboxyl radicals directly attached to carbocyclic rings
Applicants:
SANOFI-AVENTIS [FR/FR]; 174 avenue de France F-75013 Paris, FR (AllExceptUS)
GESSLER, Simon [DE/DE]; DE (UsOnly)
GILL, Harpal S. [US/US]; US (UsOnly)
LEE, George E. [US/US]; US (UsOnly)
PLETTENBURG, Oliver [DE/DE]; DE (UsOnly)
PODESCHWA, Michael [DE/DE]; DE (UsOnly)
POWERS, Matthew R. [US/US]; US (UsOnly)
ROSSEN, Kai [DE/DE]; DE (UsOnly)
SHRIMP, II, Frederick L. [US/US]; US (UsOnly)
SUBOTKOWSKI, Witold [US/US]; US (UsOnly)
VANASSE, Benoit J. [CA/US]; US (UsOnly)
WEHLAN, Hermut A. [DE/DE]; DE (UsOnly)
WEIBERTH, Franz J. [US/US]; US (UsOnly)
YU, Yong [CN/US]; US (UsOnly)
ZHANG, Jiuqing [CN/CN]; CN (UsOnly)
Inventors:
GESSLER, Simon; DE
GILL, Harpal S.; US
LEE, George E.; US
PLETTENBURG, Oliver; DE
PODESCHWA, Michael; DE
POWERS, Matthew R.; US
ROSSEN, Kai; DE
SHRIMP, II, Frederick L.; US
SUBOTKOWSKI, Witold; US
VANASSE, Benoit J.; US
WEHLAN, Hermut A.; DE
WEIBERTH, Franz J.; US
YU, Yong; US
ZHANG, Jiuqing; CN
Agent:
KURYS, Barbara, E.; Sanofi-aventis U.S. Inc. 1041 Route 202-206 Mail Code: BWD-303A Bridgewater, NJ 08807, US
Priority Data:
08291152.008.12.2008EP
095536030.07.2009FR
095542431.07.2009FR
61/120,81908.12.2008US
61/120,82408.12.2008US
Title (EN) INTERMEDIATES AND PROCESSES FOR THE PREPARATION OF FLUOROGLYCOSIDE DERIVATIVES
(FR) INTERMÉDIAIRES ET PROCÉDÉS POUR LA PRÉPARATION DE DÉRIVÉS DE FLUOROGLYCOSIDE
Abstract:
(EN) The present invention provides processes for producing (2S,3R,4R,5S,6R)-5-fluoro-6- hydroxymethyl-2-[4-(4-methoxy-benzyl)-5-trifluoromethyl-1H-pyrazol-3-yloxy]- tetrahydro-pyran-3,4-diol or a tautomer or hydrate thereof, of high purity and in a relatively high yield suitable for use on an industrial scale. The present invention is also directed to synthetic intermediates that are useful for the preparation of (2S,3R,4R,5S,6R)-5-fluoro-6-hydroxymethyl-2-[4-(4-methoxy- benzyl)-5-trifluoromethyl-1H-pyrazol-3-yloxy]-tetrahydro-pyran-3,4-diol or a tautomer or hydrate thereof.
(FR) La présente invention porte sur des procédés pour la production de (2S,3R,4R,5S,6R)-5-fluoro-6-hydroxyméthyl-2-[4-(4-méthoxybenzyl)-5-trifluorométhyl-1H-pyrazol-3-yloxy]tétrahydropyran-3,4-diol ou d'un tautomère ou un hydrate de celui-ci, de pureté élevée et avec un rendement de production relativement élevé appropriés pour être utilisés à une échelle industrielle. La présente invention porte également sur des intermédiaires de synthèse qui sont utiles pour la préparation de (2S,3R,4R,5S,6R)-5-fluoro-6-hydroxyméthyl-2-[4-(4-méthoxybenzyl)-5-trifluorométhyl-1H-pyrazol-3-yloxy]tétrahydropyran-3,4-diol ou d'un tautomère ou un hydrate de celui-ci.
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, 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 (ARIPO) (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, 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)