SG11201406945QA - Process for the preparation of 2-deoxy-2-fluoro-2-methyl-d-ribofuranosyl nucleoside compounds - Google Patents

Process for the preparation of 2-deoxy-2-fluoro-2-methyl-d-ribofuranosyl nucleoside compounds

Info

Publication number
SG11201406945QA
SG11201406945QA SG11201406945QA SG11201406945QA SG11201406945QA SG 11201406945Q A SG11201406945Q A SG 11201406945QA SG 11201406945Q A SG11201406945Q A SG 11201406945QA SG 11201406945Q A SG11201406945Q A SG 11201406945QA SG 11201406945Q A SG11201406945Q A SG 11201406945QA
Authority
SG
Singapore
Prior art keywords
international
deoxy
fluoro
south carolina
preparation
Prior art date
Application number
SG11201406945QA
Inventor
Robert Carr
Stefan Hildbrand
Mark L Hodges
Michael Kammerer
John F Lang
Iii William J Lawrimore
Dieu Nguyen
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of SG11201406945QA publication Critical patent/SG11201406945QA/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives

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.
SG11201406945QA 2012-05-29 2013-05-27 Process for the preparation of 2-deoxy-2-fluoro-2-methyl-d-ribofuranosyl nucleoside compounds SG11201406945QA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12169760 2012-05-29
PCT/EP2013/060836 WO2013178571A1 (en) 2012-05-29 2013-05-27 Process for the preparation of 2-deoxy-2-fluoro-2-methyl-d-ribofuranosyl nucleoside compounds

Publications (1)

Publication Number Publication Date
SG11201406945QA true SG11201406945QA (en) 2014-12-30

Family

ID=48520966

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201406945QA SG11201406945QA (en) 2012-05-29 2013-05-27 Process for the preparation of 2-deoxy-2-fluoro-2-methyl-d-ribofuranosyl nucleoside compounds

Country Status (19)

Country Link
US (1) US20130324709A1 (en)
EP (1) EP2855497B1 (en)
JP (1) JP2015518017A (en)
KR (1) KR20150018524A (en)
CN (1) CN104379591A (en)
AR (1) AR091166A1 (en)
AU (1) AU2013269799A1 (en)
BR (1) BR112014028692A2 (en)
CA (1) CA2872171A1 (en)
ES (1) ES2583375T3 (en)
HK (1) HK1207384A1 (en)
IL (1) IL234673A0 (en)
MX (1) MX2014014087A (en)
NZ (1) NZ631182A (en)
PT (1) PT2855497T (en)
RU (1) RU2014149148A (en)
SG (1) SG11201406945QA (en)
WO (1) WO2013178571A1 (en)
ZA (1) ZA201407529B (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USD761840S1 (en) 2011-06-28 2016-07-19 Google Inc. Display screen or portion thereof with an animated graphical user interface of a programmed computer system
CN104817599B (en) * 2015-03-20 2018-02-27 南京欧信医药技术有限公司 A kind of synthetic method of 5 hydroxyl tetrahydrofuran derivative
CN105017183B (en) * 2015-07-16 2018-06-12 江苏福瑞生物医药有限公司 A kind of method for crystallising of pharmaceutical intermediate
CN105061535A (en) * 2015-09-02 2015-11-18 江苏科本医药化学有限公司 Synthetic method of sofosbuvir intermediate
CN107805266A (en) * 2016-09-09 2018-03-16 上海度德医药科技有限公司 Preparation method as the methyl deoxyribonucleoside of 2 fluorine 2 of Suo Feibuwei intermediates
CN107629099B (en) * 2017-07-26 2020-05-26 江苏科本药业有限公司 Preparation process of sofosbuvir intermediate
CN109422781B (en) * 2017-08-25 2022-01-18 江苏瑞科医药科技有限公司 Preparation method of (2R) -2-deoxy-2-fluoro-2-methyl-D-ribofuranosyl chloride
CN109422789A (en) * 2017-08-28 2019-03-05 常州制药厂有限公司 A kind of preparation process amelioration method of Suo Feibuwei
CN109438537A (en) * 2018-11-20 2019-03-08 江苏科本药业有限公司 A kind of preparation method of Suo Feibuwei key intermediate
CN111269282A (en) * 2020-03-20 2020-06-12 江苏阿尔法药业有限公司 Method for preparing sofosbuvir intermediate by using continuous flow microchannel reactor
WO2024030429A1 (en) * 2022-08-01 2024-02-08 The United States Government, As Represented By The Secretary Of The Army Base-modified ribonucleosides as prodrugs against viral and bacterial infections

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3109244T3 (en) * 2004-09-14 2019-09-30 Gilead Pharmasset Llc Preparation of 2'fluoro-2'-alkyl-substituted or other optionally substituted ribofuranosyl pyrimidines and purines and their derivatives
WO2007065829A1 (en) * 2005-12-09 2007-06-14 F. Hoffmann-La Roche Ag Antiviral nucleosides
PT2084174E (en) * 2006-10-10 2013-10-08 Hoffmann La Roche Preparation of nucleosides ribofuranosyl pyrimidines
CN101024667B (en) * 2007-03-30 2011-01-26 湖北益泰药业有限公司 Method for preparing gemcitabine hydrochloride
EP2048151A1 (en) * 2007-10-10 2009-04-15 Cilag AG Method for producing nucleosides by direct glycosylation of the nucleoside base
US8173621B2 (en) * 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
AU2009329867B2 (en) * 2008-12-23 2015-01-29 Gilead Pharmasset Llc Nucleoside phosphoramidates

Also Published As

Publication number Publication date
US20130324709A1 (en) 2013-12-05
NZ631182A (en) 2015-09-25
AU2013269799A1 (en) 2014-10-02
WO2013178571A1 (en) 2013-12-05
MX2014014087A (en) 2015-01-26
CA2872171A1 (en) 2013-12-05
JP2015518017A (en) 2015-06-25
EP2855497B1 (en) 2016-04-20
KR20150018524A (en) 2015-02-23
ZA201407529B (en) 2015-12-23
ES2583375T3 (en) 2016-09-20
IL234673A0 (en) 2014-11-30
BR112014028692A2 (en) 2017-06-27
RU2014149148A (en) 2016-07-20
PT2855497T (en) 2016-07-28
EP2855497A1 (en) 2015-04-08
AR091166A1 (en) 2015-01-14
HK1207384A1 (en) 2016-01-29
CN104379591A (en) 2015-02-25

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