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1. (WO2010083722) A PROCESS FOR ONE-POT SYNTHESIS OF COREY LACTONE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/083722 International Application No.: PCT/CN2010/000058
Publication Date: 29.07.2010 International Filing Date: 13.01.2010
IPC:
C07D 307/935 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77
ortho- or peri-condensed with carbocyclic rings or ring systems
93
condensed with a ring other than six-membered
935
Not further condensed cyclopenta [b] furans or hydrogenated cyclopenta [b] furans
Applicants:
中国药科大学 CHINA PHARMACEUTICAL UNIVERSITY [CN/CN]; 中国江苏省南京市童家巷24号 No.24 Tongjiaxiang Nanjing Jiangsu 210009, CN (AllExceptUS)
合肥医工医药有限公司 HEFEI YIGONG MEDICINE CO., LTD. [CN/CN]; 中国安徽省合肥市长江西路669号高新区创业中心F8楼 F8, Innovation Center High & New Zone No. 669, Changjiang West Road Hefei, Anhui 230088, CN (AllExceptUS)
孙宏斌 SUN, Hongbin [CN/CN]; CN (UsOnly)
龚彦春 GONG, Yanchun [CN/CN]; CN (UsOnly)
侯英伟 HOU, Yingwei [CN/CN]; CN (UsOnly)
何广卫 HE, Guangwei [CN/CN]; CN (UsOnly)
Inventors:
孙宏斌 SUN, Hongbin; CN
龚彦春 GONG, Yanchun; CN
侯英伟 HOU, Yingwei; CN
何广卫 HE, Guangwei; CN
Agent:
南京知识律师事务所 ZHISHI LAW FIRM OF INTELLECTUAL PROPERTY; 中国江苏省南京市新模范马路5号南京科技广场B座9楼 9F, Block B, Nanjing Sci-Tech Center No. 5 Xinmofan Road, Nanjing Jiangsu 210009, CN
Priority Data:
200910028164.420.01.2009CN
Title (EN) A PROCESS FOR ONE-POT SYNTHESIS OF COREY LACTONE
(FR) PROCÉDÉ DE SYNTHÈSE MONOTOPE DE LA LACTONE DE COREY
(ZH) 一锅煮方法合成COREY内酯的工艺
Abstract:
(EN) A process for one-pot synthesis of Corey lactone, characterized in that it comprises selecting 2-halo-5-oxobicyclo[2.2.1]heptane-7-carboxylic acid and ester derivatives having the formula I as raw material, adding oxidant, alkalizing with base, acidifying with acid, completing the oxidation of material, ring-opening, cyclization continuously in the same reactor, and purifying to obtain the production 5-hydroxy-hexahydro-2-oxo-2H-cyclopenta[b]furan-4-carboxylic acid having the formula II, i.e. Corey lactone. In the process for one-pot synthesis of Corey lactone having the formula II, Corey lactone is easy to be resolved and is the key intermediate for synthesis of prostaglandins. The method is simple to operate and the raw materials are cheap and easy to be obtained. The method has low pollution to environment and can reduce the cost for producing Corey lactone with large range.
(FR) L'invention concerne un procédé de synthèse monotope de la lactone de Corey, caractérisé en ce qu'il comprend la sélection de l'acide 2-halogéno-5-oxobicyclo[2.2.1]heptane-7-carboxylique et ses dérivés ester de formule I en tant matière première, l'ajout d'un oxydant, une alcalinisation avec une base, une acidification avec un acide, la terminaison de l'oxydation du matériau, une ouverture de cycle, une cyclisation en continu dans le même réacteur, et une purification pour obtenir l'acide 5-hydroxy-hexahydro-2-oxo-2H-cyclopenta[b]furane-4-carboxylique de formule II, c.-à-d. la lactone de Corey. Selon le procédé de synthèse monotope de la lactone de Corey de formule II, la lactone de Corey est facile à séparer et est l'intermédiaire clé pour la synthèse de prostaglandines. Le procédé est simple à mettre en œuvre et les matières premières sont peu coûteuses et faciles à obtenir. Le procédé ne pollue pas l'environnement et peut réduire le coût de production de la lactone de Corey dans une large mesure.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, 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, PE, PG, PH, PL, PT, RO, RS, RU, 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 (ARIPO) (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, MK, MT, NL, NO, PL, PT, RO, 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)