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Pub. No.:    WO/2010/027113    International Application No.:    PCT/KR2008/005239
Publication Date: 11.03.2010 International Filing Date: 04.09.2008
C07D 211/90 (2006.01), C07D 213/80 (2006.01)
Applicants: AHN-GOOK PHARMACEUTICAL CO., LTD [KR/KR]; #993-75, Daelim-dong Yongdungpo-ku Seoul 150-953 (KR) (For All Designated States Except US).
KOREA ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY [KR/KR]; 373-1, Guseong-dong, Yuseong-gu, Daejeon 305-701 (KR) (For All Designated States Except US).
AUH, Jin [KR/KR]; (KR) (For US Only).
WON, Duk Kwon [KR/KR]; (KR) (For US Only).
MOON, Byung Hyun [KR/KR]; (KR) (For US Only).
KWON, O Zoon [KR/KR]; (KR) (For US Only).
JONG, Chang Woo [KR/KR]; (KR) (For US Only).
JIN, Kyung Yong [KR/KR]; (KR) (For US Only).
BAE, Kyoung Ho [KR/KR]; (KR) (For US Only).
LEE, Hee Yoon [KR/KR]; (KR) (For US Only).
SHIN, Jung Ah [KR/KR]; (KR) (For US Only)
Inventors: AUH, Jin; (KR).
WON, Duk Kwon; (KR).
MOON, Byung Hyun; (KR).
KWON, O Zoon; (KR).
JONG, Chang Woo; (KR).
JIN, Kyung Yong; (KR).
BAE, Kyoung Ho; (KR).
LEE, Hee Yoon; (KR).
SHIN, Jung Ah; (KR)
Agent: YOON & YANG; 11th Floor, Namkang Bldg. 1340-6, Seocho-dong Seocho-gu Seoul 137-861 (KR)
Priority Data:
Abstract: front page image
(EN)The embodiment proposes a method for preparing (S)-(-)- ethyl methyl 4-(2,3-dichlorophenyl)- 1,4-dihydro-2,6-dimethyl-3,5-pyridine- dicarboxylate (hereinafter, referring to as "(S)-(-)-felodipine", and more particularly, a method for effectively preparing the (S)-(-)-felodipine through a selective transesterification of -hydroxy ester after synthesizing a felodipine derivate including a chiral separation compound and isolating (S)-isomers. The chiral separation compound is synthesized from (R)-glycidol or (S)-glycidol through reaction with various nucleophiles and epoxide.
(FR)Un mode de réalisation de la présente invention concerne un procédé de préparation de (S)-(-)- éthyle méthyle 4-(2,3-dichlorophényl)-1,4-dihydro-2,6-diméthyl-3,5-pyridine-dicarboxylate (appelé "(S)-(-)-félodipine"), et plus particulièrement un procédé de préparation efficace de (S)-(-)-félodipine par le biais d'une transestérification sélective d'hydroxyester après synthèse d'un dérivé de félodipine contenant un composé de séparation chirale et isolement de (S)-isomères. Le composé de séparation chirale est synthétisé à partir de (R)-glycidol ou de (S)-glycidol par réaction avec divers nucléophiles et de l'époxyde.
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: English (EN)
Filing Language: Korean (KO)