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1. (WO2018159639) METHOD FOR PRODUCING HETEROCYCLIC COMPOUND
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Pub. No.: WO/2018/159639 International Application No.: PCT/JP2018/007349
Publication Date: 07.09.2018 International Filing Date: 27.02.2018
IPC:
C07D 405/14 (2006.01) ,C07D 231/12 (2006.01) ,C07D 405/10 (2006.01) ,A61K 31/4155 (2006.01) ,A61P 25/28 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02
not condensed with other rings
10
having two or three double bonds between ring members or between ring members and non-ring members
12
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
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
415
1,2-Diazoles
4155
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25
Drugs for disorders of the nervous system
28
for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Applicants:
武田薬品工業株式会社 TAKEDA PHARMACEUTICAL COMPANY LIMITED [JP/JP]; 大阪府大阪市中央区道修町四丁目1番1号 1-1, Doshomachi 4-chome, Chuo-ku, Osaka-shi, Osaka 5410045, JP
Inventors:
兼松 誠 KANEMATSU, Makoto; JP
石本 和久 ISHIMOTO, Kazuhisa; JP
加▲藤▼ 友祥 KATOU, Tomoaki; JP
Agent:
高島 一 TAKASHIMA, Hajime; JP
鎌田 光宜 KAMADA, Mitsunori; JP
Priority Data:
2017-03689828.02.2017JP
Title (EN) METHOD FOR PRODUCING HETEROCYCLIC COMPOUND
(FR) PROCÉDÉ DE PRODUCTION DE COMPOSÉ HÉTÉROCYCLIQUE
(JA) 複素環化合物の製造方法
Abstract:
(EN) Provided is a method for producing a heterocyclic compound which is useful as a prophylactic and/or therapeutic agent for Alzheimer's disease and the like. A method for producing 1,5-anhydro-2,4-dideoxy-2-(4-fluoro-5-methyl-1-oxo-6-(4-(1H-pyrazol-1-yl)benzyl)-1,3-dihydro-2H-isoindol-2-yl)-L-threo-pentitol or a salt thereof, comprising reacting 4-fluoro-3-hydroxy-5-methyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2-benzofuran-1(3H)-one or a salt thereof, 3-fluoro-2-formyl-4-methyl-5-[4-(1H-pyrazol-1-yl)benzyl]benzoic acid or a salt thereof, or a mixture thereof with 2-amino-1,5-anhydro-2,4-dideoxy-L-threo-pentitol.
(FR) L'invention concerne un procédé de production d'un composé hétérocyclique qui est utile en tant qu'agent prophylactique et/ou thérapeutique pour la maladie d'Alzheimer et similaire. L'invention concerne un procédé de production de 1,5-anhydro-2,4-didésoxy-2-(4-fluoro-5-méthyl-1-oxo-6-(4-(1H-pyrazol-1-yl)benzyl)-1,3-dihydro-2H-isoindol-2-yl)-L-thréo-pentitol ou un sel de celui-ci, comprenant la mise en réaction de 4-fluoro-3-hydroxy-5-méthyl-6-[4-(1H-pyrazol-1-yl)benzyl]-2-benzofuran-1(3H)-one ou un sel de celui-ci, l'acide benzoïque 3-fluoro-2-formyl-4-méthyl-5-[4-(1H-pyrazol-1-yl) benzyl] ou un sel de celui-ci, ou un mélange de ceux-ci avec du 2-amino-1,5-anhydro-2,4-didésoxy-L-thréo-pentitol.
(JA) アルツハイマー病等の予防および/または治療薬として有用な複素環化合物の製造方法を提供すること。4-フルオロ-3-ヒドロキシ-5-メチル-6-[4-(1H-ピラゾール-1-イル)ベンジル]-2-ベンゾフラン-1(3H)-オンもしくはその塩、 3-フルオロ-2-ホルミル-4-メチル-5-[4-(1H-ピラゾール-1-イル)ベンジル]安息香酸もしくはその塩、 またはその混合物を、 2-アミノ-1,5-アンヒドロ-2,4-ジデオキシ-L-トレオ-ペンチトールと反応させることを含む、 1,5-アンヒドロ-2,4-ジデオキシ-2-(4-フルオロ-5-メチル-1-オキソ-6-(4-(1H-ピラゾール-1-イル)ベンジル)-1,3-ジヒドロ-2H-イソインドール-2-イル)-L-トレオ-ペンチトールまたはその塩の製造方法。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, 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, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)