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1. (WO2013152608) METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2013/152608    International Application No.:    PCT/CN2012/087732
Publication Date: 17.10.2013 International Filing Date: 27.12.2012
IPC:
C07D 475/04 (2006.01)
Applicants: ASYMCHEM LABORATORIES (TIANJIN) CO., LTD [CN/CN]; No. 6 Dongting 3rd Street Teda Tianjin 300457 (CN) (For All Designated States Except US).
ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD [CN/CN]; No. 71, 7th Street Teda Tianjin 300457 (CN) (For All Designated States Except US).
TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD [CN/CN]; Teda Tianjin 300000 (CN) (For All Designated States Except US).
ASYMCHEM LABORATORIES (FUXIN) CO., LTD [CN/CN]; No. 42 E Road, Economic and Technological Development Zone Fuxin, Liaoning 123000 (CN) (For All Designated States Except US).
JILIN ASYMCHEM LABORATORIES CO.,LTD [CN/CN]; Industrial Park, Economic and Technological Development Zone Dunhua, Jilin 133700 (CN) (For All Designated States Except US).
HONG, Hao [US/CN]; (CN) (US only).
GAGE, James [US/CN]; (CN) (US only).
CHEN, Chaoyong [CN/CN]; (CN) (US only).
LU, Jiangping [CN/CN]; (CN) (US only).
ZHOU, Yan [CN/CN]; (CN) (US only).
LIU, Shuangyong [CN/CN]; (CN) (US only)
Inventors: HONG, Hao; (CN).
GAGE, James; (CN).
CHEN, Chaoyong; (CN).
LU, Jiangping; (CN).
ZHOU, Yan; (CN).
LIU, Shuangyong; (CN)
Agent: KANGXIN PARTNERS, P.C.; Floor 16, Tower A, Indo Building A48 Zhichun Road, Haidian District Beijing 100098 (CN)
Priority Data:
201210102879.1 10.04.2012 CN
Title (EN) METHOD FOR SYNTHESIZING SAPROPTERIN DIHYDROCHLORIDE
(FR) PROCÉDÉ DE SYNTHÈSE DE DICHLORHYDRATE DE SAPROPTÉRINE
(ZH) 一种二盐酸沙丙喋呤的合成方法
Abstract: front page image
(EN)Disclosed is a method for synthesizing sapropterin dihydrochloride. The present invention reduces a synthesis route of the sapropterin dihydrochloride, and resolves a racemate intermediate or an intermediage having a low antimer isomerism value by using a chiral resolving reagent, thereby obtaining an intermediate having a high antimer isomerism value. Raw materials are cheap and readily available, and the cost is significantly reduced, hence providing an effective scheme for mass industrial production of the sapropterin dihydrochloride.
(FR)L'invention concerne un procédé de synthèse de dichlorhydrate de saproptérine. La présente invention réduit une voie de synthèse du dichlorhydrate de saproptérine et sépare un intermédiaire racémate ou un intermédiaire ayant une faible valeur d'isomérisme d'antimère en utilisant un réactif de résolution chirale, ce qui permet d'obtenir un intermédiaire ayant une valeur élevée d'isomérisme d'antimère. Les matières premières sont peu coûteuses et facilement disponibles, et les coûts sont significativement réduits, ce qui permet d'obtenir un procédé efficace pour la production industrielle en masse du dichlorhydrate de saproptérine.
(ZH)本发明公开了一种二盐酸沙丙喋呤的合成方法,该发明缩短了二盐酸沙丙喋呤的合成路线,利用手性拆分试剂拆分消旋中间体或者低对映体异构值的中间体,得到高对映体异构值的中间体,原料廉价易得,大大降低了成本,为二盐酸沙丙喋呤的大规模工业化生产提供了一条行之有效的思路。
Designated States: 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, 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, 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.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)
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)