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1. (WO2007011065) INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2007/011065 International Application No.: PCT/JP2006/314932
Publication Date: 25.01.2007 International Filing Date: 21.07.2006
IPC:
C07D 265/30 (2006.01) ,C07D 265/32 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
30
not condensed with other rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
28
1,4-Oxazines; Hydrogenated 1,4-oxazines
30
not condensed with other rings
32
with oxygen atoms directly attached to ring carbon atoms
Applicants:
MITSUBISHI TANABE PHARMA CORPORATION [JP/JP]; 2-10, Dosho-machi 3-chome Chuo-ku, Osaka-shi Osaka 5418505, JP (AllExceptUS)
SANOFI-AVENTIS [FR/FR]; 174, avenue de France, Paris F-75013, FR (AllExceptUS)
OKUYAMA, Masahiro [JP/JP]; JP (UsOnly)
UEHARA, Fumiaki [JP/JP]; JP (UsOnly)
IWAMURA, Hiroshi [JP/JP]; JP (UsOnly)
WATANABE, Kazutoshi [JP/JP]; JP (UsOnly)
Inventors:
OKUYAMA, Masahiro; JP
UEHARA, Fumiaki; JP
IWAMURA, Hiroshi; JP
WATANABE, Kazutoshi; JP
Agent:
TAKASHIMA, Hajime; Meiji Yasuda Seimei Osaka Midosuji Bldg. 1-1, Fushimimachi 4-chome Chuo-ku, Osaka-shi Osaka 541-0044, JP
Priority Data:
2005-21331122.07.2005JP
2005-26748514.09.2005JP
2006-01543624.01.2006JP
Title (EN) INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF
(FR) COMPOSE INTERMEDIAIRE UTILISE POUR LA SYNTHESE D'UN AGENT PHARMACEUTIQUE, PROCEDE DE PRODUCTION DE CE DERNIER
Abstract:
(EN) The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
(FR) La présente invention concerne un procédé de production d'un composé morpholine optiquement actif représenté par la formule (10) qui comprend les étapes suivantes dans lesquelles chaque symbole est tel que défini dans le descriptif. Cette invention porte également sur un procédé de production d'un composé représenté par la formule (55) qui comprend les étapes suivantes dans lesquelles chaque symbole est tel que spécifié dans le descriptif. Conformément au procédé de production selon l'invention, un composé morpholine à substitution 2 aryle optiquement actif et un 3-oxo-3-(pyrimidin-4-yl)propionate qui sont importants en tant que produits de départ pour la synthèse de 2-(2-arylmorpholin-4-yl)-1-méthyl-1H-[4,4']bipyrimidinyl-6-one présentant une activité inhibitrice de la tau protéine kinase 1 et utile en tant que médicament thérapeutique pour la maladie d'Alzheimer et similaire peuvent être produits à haut rendement par un procédé avantageux du point de vue industriel. Formule (10)
front page image
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:
NO20080914MXMX/a/2008/000996KR1020080030675IL188786EP2221304EP2221305
EP1910320ZA2008/01589JP2009502733US20090156804CN101228142CA2615515
EA200800401NZ566009AU2006270742IN880/CHENP/2008