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1. (WO2007009143) METHOD FOR PRODUCING NEBIVOLOL
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/009143 International Application No.: PCT/AT2006/000303
Publication Date: 25.01.2007 International Filing Date: 17.07.2006
IPC:
C07D 311/58 (2006.01) ,C07F 7/18 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
311
Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02
ortho- or peri-condensed with carbocyclic rings or ring systems
04
Benzo [b] pyrans, not hydrogenated in the carbocyclic ring
58
other than with oxygen or sulfur atoms in position 2 or 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
7
Compounds containing elements of the 4th Group of the Periodic System
02
Silicon compounds
08
Compounds having one or more C-Si linkages
18
Compounds having one or more C-Si linkages as well as one or more C-O-Si linkages
Applicants:
PHARMACON - FORSCHUNG UND BERATUNG GMBH [AT/AT]; Riglergasse 4 A-1180 Wien, AT (AllExceptUS)
NOE, Christian, R. [AT/AT]; AT (UsOnly)
JASIC, Muhamed; AT (UsOnly)
KOLLMANN, Hermann; AT (UsOnly)
LACHMANN, Bodo; DE (UsOnly)
Inventors:
NOE, Christian, R.; AT
JASIC, Muhamed; AT
KOLLMANN, Hermann; AT
LACHMANN, Bodo; DE
Agent:
BEER, Manfred ; Lindengasse 8 A-1070 Wien, AT
Priority Data:
A1214/200519.07.2005AT
Title (DE) VERFAHREN ZUR HERSTELLUNG NEBIVOLOL
(EN) METHOD FOR PRODUCING NEBIVOLOL
(FR) PROCEDE DE PRODUCTION DE NEBIVOLOL
Abstract:
(DE) Gegenstand der Erfindung ist ein Verfahren zur Herstellung des razernischen Wirkstoffes Nebivolol, vorzugsweise als Hydrochlorid gemäß Formel (I) bei welchem diastereomere Cyanhydrine der allgemeinen Formel (II) hergestellt, getrennt und die getrennten Diastereomere nach einer Transformation, vorzugsweise einer teilweisen oder vollen Reduktion der Cyanogruppe oder einer Pinner-Verseifung, miteinander gekoppelt werden.
(EN) The invention relates to a method for producing the racemic active ingredient Nebivolol, preferably in the form of the hydrochloride of formula (1), according to which diastereomer cyanhydrins of general formula (2) are produced and separated, and the separated diastereomers are coupled together following a transformation, preferably a partial or full reduction of the cyano group or a Pinner saponification.
(FR) L'invention concerne un procédé permettant de produire le principe actif racémique Nébivolol, selon lequel des cyanhydrines diastéréomères sont produites, séparées et les diastéréomères séparés sont à nouveau accouplés, après une transformation, de préférence une réduction partielle ou complète du groupe cyano ou une saponification de Pinner.
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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: German (DE)
Filing Language: German (DE)
Also published as:
NO20080823NZ565573MXMX/a/2008/000747KR1020080027368IL188777EP1919888
BRPI0613610-9ZA2008/00963JP2009502750US20080221340CN101243062CA2615832
EA200800364AU2006272420ID048.2015IN186/KOLNP/2008