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1. (WO2007003522) METHOD FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND, SYNTHESIS INTERMEDIATES THEREOF AND METHODS FOR OBTAINING THEM
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/003522 International Application No.: PCT/EP2006/063534
Publication Date: 11.01.2007 International Filing Date: 26.06.2006
Chapter 2 Demand Filed: 14.11.2006
IPC:
C07D 451/14 (2006.01) ,C07D 471/18 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
451
Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
14
containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12
in which the condensed system contains three hetero rings
18
Bridged systems
Applicants:
INKE, S.A. [ES/ES]; Pol. Ind. Can Pelegrí - C. Argent 1 E-08755 Castellbisbal, ES (AllExceptUS)
PEREZ ANDRES, Juan Antonio [ES/ES]; ES (UsOnly)
DALMASES BARJOAN, Pere [ES/ES]; ES (UsOnly)
Inventors:
PEREZ ANDRES, Juan Antonio; ES
DALMASES BARJOAN, Pere; ES
Agent:
PONTI SALES, Adelaida ; OFICINA PONTI, S.L. C. De Consell De Cent 322 E-08007 Barcelona, ES
Priority Data:
60/702,89427.07.2005US
P-20050170406.07.2005ES
Title (EN) METHOD FOR OBTAINING A PHARMACEUTICALLY ACTIVE COMPOUND, SYNTHESIS INTERMEDIATES THEREOF AND METHODS FOR OBTAINING THEM
(FR) PROCÉDÉ SERVANT À OBTENIR UN COMPOSÉ ACTIF DU POINT DE VUE PHARMACEUTIQUE, INTERMÉDIAIRES DE SYNTHÈSE DE CELUI-CI ET PROCÉDÉS SERVANT À OBTENIR CEUX-CI
Abstract:
(EN) The present invention relates to a method for obtaining Dolasetron that comprises: a) Esterification of the alcohol of formula (IV) with indole-3-carboxylic acid (compound (III)) or a reactive derivative thereof, to give a compound of formula (V), followed by step b) which includes Dieckmann reaction of the intermediate (V), by reaction with a strong organic or inorganic base, to give the intermediate (VI), and step c) which comprises dealcoxycarbonylation of the intermediate (VI) to give Dolasetron base and, if desired, a pharmaceutically acceptable salt thereof, hydrates or solvates of the base of said salt. The invention also relates to the intermediates (V) and (VI), and methods for obtaining them. With the method of the present invention Dolasetron is obtained at industrial scale with good yields, with decreased use of reactants and solvents, while said method is also of greater atomic efficiency.
(FR) La présente invention concerne un procédé servant à obtenir du Dolasétron lequel comprend : a) l'estérification de l'alcool de formule (IV) avec l'acide indole-3-carboxylique (composé (III)) ou un dérivé réactif de celui-ci, pour donner un composé de formule (V), suivie de l'étape b) qui comprend une réaction de Dieckmann sur l'intermédiaire (V), par réaction avec une base forte organique ou inorganique, pour donner l'intermédiaire (VI) et d'une étape c) qui comprend l'élimination du groupe alcoxycarbonyle de l'intermédiaire (VI) pour donner la base du Dolasétron et, si on le souhaite, un sel acceptable du point de vue pharmaceutique de celle-ci, des hydrates ou solvates de la base dudit sel. L'invention concerne également les intermédiaires (V) et (VI) et les procédés servant à obtenir ceux-ci. Avec le procédé de la présente invention on obtient du Dolasétron à l'échelle industrielle avec de bons rendements de production, avec une utilisation réduite de réactifs et de solvants, tout en ayant également un meilleur rendement atomique dudit procédé.
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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, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, SY, 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, 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: English (EN)
Filing Language: English (EN)
Also published as:
EP1904492ES2264901US20080194824