WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2007009303) PROCESS FOR SYNTHESIZING N4-ACYL-5'-DEOXY-5-FLUOROCYTIDINE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/009303    International Application No.:    PCT/CN2005/001338
Publication Date: 25.01.2007 International Filing Date: 29.08.2005
IPC:
C07H 19/067 (2006.01), C07C 69/003 (2006.01)
Applicants: SHANGHAI AURISCO INTERNATIONAL TRADING CO., LTD. [CN/CN]; Rm. 1709-1710, HiTech Plaza N0. 488 South Wuning Road Jing'an District Shanghai 200042 (CN) (For All Designated States Except US).
YU, Dihu [CN/CN]; (CN) (For US Only)
Inventors: YU, Dihu; (CN)
Agent: SHANGHAI XIN TIAN PATENT AGENT CO., LTD.; Rm 1606, No. 59, Nan Chang Road Shanghai 200020 (CN)
Priority Data:
200510027773.X 15.07.2005 CN
Title (EN) PROCESS FOR SYNTHESIZING N4-ACYL-5'-DEOXY-5-FLUOROCYTIDINE DERIVATIVES
(FR) PROCEDE DE SYNTHESE DE DERIVES DE N4-ACYL-5'-DESOXY-5-FLUOROCYTIDINE
(ZH) 合成 N⁴-酰基-5' -脱氧-5-氟胞苷衍生物的方法
Abstract: front page image
(EN)The present invention discloses a process for synthesizing Compound (I) of N4-acyl-5'-deoxy-5-fluorocytidine derivatives. The present invention utilizes Bis (trichloromethyl) carbobate as acylating agent for introducing protective lactone ring to the hydroxyl of saccharide moiety, and uses 5'-deoxy-5-fluorocytidine (Compound II) as starting material through key intermediate of Compound (III) and Compound (IV) to obtain target compounds through 3 steps. The process of the present invention has certain advantages such as high yield, short work-up time, available starting material, and convenience for industrial manufacture on a large scale.
(FR)La présente invention concerne un procédé de synthèse du composé (I) consistant en des dérivés de N4-acyl-5'-désoxy-5-fluorocytidine. Le procédé selon la présente invention utilise du bis(trichlorométhyl)carbobate en tant qu'agent d'acylation pour introduire un cycle lactone protecteur à la fonction hydroxyle du saccharide, ainsi que du 5'-désoxy-5-fluorocytidine (Composé II) en tant que matériau de départ pour obtenir les composés voulus en 3 étapes en passant par des intermédiaires clés, le composé (III) et le composé (IV). Ce procédé présente un certain nombre d'avantages, tels qu'un rendement élevé, une durée de traitement courte, un matériau de départ disponible, et il est également adapté à une fabrication industrielle à grande échelle.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, 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, HU, IE, IS, IT, LT, LU, LV, MC, NL, 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: Chinese (ZH)
Filing Language: Chinese (ZH)