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1. (WO2001030763) PROCESS FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE DERIVATIVE AND OPTICAL RESOLVER THEREFOR
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/030763 International Application No.: PCT/JP2000/007282
Publication Date: 03.05.2001 International Filing Date: 19.10.2000
Chapter 2 Demand Filed: 10.01.2001
IPC:
A61K 31/4164 (2006.01) ,C07D 233/54 (2006.01) ,C07F 9/50 (2006.01) ,C07F 9/6574 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4164
1,3-Diazoles
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
233
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
54
having two double bonds between ring members or between ring members and non-ring members
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
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
28
with one or more P-C bonds
50
Organo-phosphines
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
9
Compounds containing elements of the 5th Group of the Periodic System
02
Phosphorus compounds
547
Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
6564
having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
6571
having phosphorus and oxygen atoms as the only ring hetero atoms
6574
Esters of oxyacids of phosphorus
Applicants:
AOKI, Isao [JP/JP]; JP (UsOnly)
ADACHI, Mari [JP/JP]; JP (UsOnly)
KAWADA, Mitsuru [JP/JP]; JP (UsOnly)
YAMANO, Toru [JP/JP]; JP (UsOnly)
TAYA, Naohiro [JP/JP]; JP (UsOnly)
TAKEDA CHEMICAL INDUSTRIES, LTD. [JP/JP]; 1-1, Doschomachi 4-chome Chuo-ku Osaka-shi Osaka 541-0045, JP (AllExceptUS)
Inventors:
AOKI, Isao; JP
ADACHI, Mari; JP
KAWADA, Mitsuru; JP
YAMANO, Toru; JP
TAYA, Naohiro; JP
Agent:
TAKAHASHI, Shuichi ; Osaka Plant of Takeda Chemical Industries, Ltd. 17-85, Jusohonmachi 2-chome Yodogawa-ku Osaka-shi Osaka 532-0024, JP
Priority Data:
11/30157022.10.1999JP
11/30157622.10.1999JP
Title (EN) PROCESS FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE DERIVATIVE AND OPTICAL RESOLVER THEREFOR
(FR) PROCEDE DE PRODUCTION DE DERIVE DE NAPHTALENE OPTIQUEMENT ACTIF ET SON SEPARATEUR OPTIQUE
Abstract:
(EN) A process for producing an optically active isomer of a compound represented by formula (I) which comprises: reacting a mixture of naphthalene derivatives represented by formula (I) (wherein R represents a nitrogenous heterocyclic group; R1 represents hydrogen, a hydrocarbon group, or a mononuclear aromatic heterocyclic group; R2 represents hydrogen or lower alkyl; symbol * indicates the position of an asymmetric carbon atom; and R3 to R8 each represents hydrogen, a hydrocarbon group, hydroxy, etc., provided that R7 may be bonded to R6 or R8 to form a ring containing an oxygen atom) with an optically active isomer of a compound represented by formula (II) or (III) (wherein ring A represents a benzene ring; R10 and R11 each represents hydrogen, a hydrocarbon group, etc. or R10 and R11 in combination represent alkylene; symbol * indicates the position of an asymmetric carbon atom; and rings B and C each represents an aromatic ring) to yield salts; separating the salts; and then isolating the target isomer. The optically active isomer produced has a steroid C17,20 lyase inhibitory activity and is useful as a preventive/remedy for tumors such as prostatism and mammary cancer. Also provided is a novel optical resolver.
(FR) La présente invention concerne un procédé de production de l'isomère optiquement actif d'un composé de formule (I) consistant à: (a) faire réagir le mélange de dérivés de naphtalène représentés par la formule (I), (dans laquelle R représente un groupe hétérocyclique azoté; R1 représente hydrogène, un groupe d'hydrocarbures, ou un groupe hétérocyclique aromatique mononucléaire; R2 représente hydrogène ou alkyle inférieur; le symbole * indique la position d'un atome de carbone asymétrique; et R3 à R8 représentent chacun hydrogène, un groupe d'hydrocarbures, hydroxy, etc., à condition que R7 puisse être lié à R6 ou R8 pour former un noyau contenant un atome d'oxygène), avec l'isomère optiquement actif d'un composé représenté par la formule (II) ou (III), (dans laquelle le noyau A représente un noyau benzénique; R10 et R11 représentent chacun hydrogène, un groupe d'hydrocarbures, etc., ou R10 et R11 associés représentent alkylène; le symbole * indique la position d'un atome de carbone asymétrique; les noyaux B et C représentent chacun un noyau aromatique) pour obtenir des sels; (b) séparer les sels; et enfin, (c) isoler l'isomère cible. L'isomère optiquement actif produit présente une activité inhibitrice lyase stéroïde C17,20 celui-ci étant utilisé pour prévenir/traiter les tumeurs telles que le cancer de la prostate et du sein. En outre, cette invention concerne un nouveau séparateur optique.
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Designated States: AE, AG, AL, AM, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CN, CR, CU, CZ, DM, DZ, EE, GD, GE, HR, HU, ID, IL, IN, IS, JP, KG, KR, KZ, LC, LK, LR, LT, LV, MA, MD, MG, MK, MN, MX, NO, NZ, PL, RO, RU, SG, SI, SK, TJ, TM, TR, TT, UA, US, UZ, VN, YU, ZA
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)