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1. (WO2009062377) RESOLUTION OF 4,5-DIMETHOXY-1-(METHYLAMINOMETHYL)-BENZOCYCLOBUTANE
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2009/062377    International Application No.:    PCT/CN2008/001711
Publication Date: 22.05.2009 International Filing Date: 10.10.2008
IPC:
C07C 217/54 (2006.01), C07C 213/08 (2006.01), C07D 223/16 (2006.01)
Applicants: JIANGSU HENGRUI MEDICINE CO. LTD. [CN/CN]; No.145 East Renmin Road Xinpu District Lianyungang, Jiangsu 222002 (CN) (For All Designated States Except US).
SUN, Piaoyang [CN/CN]; (CN) (For US Only).
CHEN, Yongjiang [CN/CN]; (CN) (For US Only).
YU, Guangliang [CN/CN]; (CN) (For US Only)
Inventors: SUN, Piaoyang; (CN).
CHEN, Yongjiang; (CN).
YU, Guangliang; (CN)
Agent: GE CHENG & CO., LTD.; Level 19, Tower E3, The Towers Oriental Plaza, No.1, East Chang An Avenue Dongcheng District Beijing 100738 (CN)
Priority Data:
200710188301.1 16.11.2007 CN
200810093266.X 19.05.2008 CN
Title (EN) RESOLUTION OF 4,5-DIMETHOXY-1-(METHYLAMINOMETHYL)-BENZOCYCLOBUTANE
(FR) RÉSOLUTION DE 4,5-DIMÉTHOXY-1-(MÉTHYLAMINOMÉTHYL)-BENZOCYCLOBUTANE
(ZH) 4,5-二甲氧基-1-(甲基氨基甲基)-苯并环丁烷的拆分
Abstract: front page image
(EN)A method of resolution of an important chemical intermediate, 4,5-dimethoxy-1-(methylaminomethyl)-benzocyclobutane, comprises the following steps: reacted its two enantiomers of 4,5-dimethoxy-1-(methylaminomethyl)-benzocyclobutane with di-p-toluoyl-L-tartaric acid (L-DTTA) or di-p-toluoyl-D-tartaric acid (D-DTTA) in a solution of alcohol or alcohol in water to give its salts, then resolved the salts. This gives high enantiomer excess value, high yield which is more than 80% in total with normal separation and reversed separation.
(FR)L'invention concerne un procédé de résolution d'un intermédiaire chimique important, le 4,5-diméthoxy-1-(méthylaminométhyl)-benzocyclobutane, qui comprend les étapes suivantes : mise en réaction des deux énantiomères du 4,5-diméthoxy-1-(méthylaminométhyl)-benzocyclobutane avec l'acide di-p-toluoyl-L-tartarique (L-DTTA) ou l'acide di-p-toluoyl-D-tartarique (D-DTTA) dans une solution d'alcool ou d'alcool dans de l'eau pour obtenir leurs sels, puis résolution des sels. Ceci permet d'obtenir une valeur d'excès énantiomérique élevée, un rendement élevé supérieur à 80 % au total avec la séparation normale et la séparation inversée.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, 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, 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 (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, MT, NL, NO, 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)