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1. (WO2018199040) METHOD FOR MANUFACTURING DIASTEREOMER OF CITRIC ACID DERIVATIVE
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Pub. No.: WO/2018/199040 International Application No.: PCT/JP2018/016495
Publication Date: 01.11.2018 International Filing Date: 23.04.2018
IPC:
C07D 207/416 (2006.01) ,A61K 31/4015 (2006.01) ,A61P 1/16 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
207
Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
30
having two double bonds between ring members or between ring members and non-ring members
34
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
36
Oxygen or sulfur atoms
40
2,5-Pyrrolidine-diones
416
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to other ring carbon atoms
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
40
having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
4015
having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1
Drugs for disorders of the alimentary tract or the digestive system
16
for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
Applicants:
株式会社大塚製薬工場 OTSUKA PHARMACEUTICAL FACTORY, INC. [JP/JP]; 徳島県鳴門市撫養町立岩字芥原115 115, Aza Kuguhara, Tateiwa, Muya-cho, Naruto-shi, Tokushima 7728601, JP
AdaBio株式会社 ADABIO CO.,LTD. [JP/JP]; 群馬県高崎市剣崎町21番地2 21-2, Kenzaki-machi, Takasaki-shi, Gunma 3700883, JP
Inventors:
平石 勝也 HIRAISHI, Katsuya; JP
相馬 洋之 SOMA, Hiroyuki; JP
神間 史恵 JIMMA, Fumie; JP
足立 太郎 ADACHI, Taro; JP
山岡 一平 YAMAOKA, Ippei; JP
遠藤 直之 ENDO, Naoyuki; JP
Agent:
廣田 雅紀 HIROTA, Masanori; JP
Priority Data:
2017-08972528.04.2017JP
Title (EN) METHOD FOR MANUFACTURING DIASTEREOMER OF CITRIC ACID DERIVATIVE
(FR) PROCÉDÉ DE FABRICATION DE DIASTÉRÉOISOMÈRE D'UN DÉRIVÉ D'ACIDE CITRIQUE
(JA) クエン酸誘導体のジアステレオマーの製造方法
Abstract:
(EN) By performing ion exchange column chromatography on an aqueous solution containing a compound A represented by formula (A) and citric acid or by treating the aqueous solution with calcium carbonate, the citric acid in the aqueous solution is removed, and a crystalline compound A is obtained by subsequently subjecting the aqueous solution to several steps. In addition, a high-purity, non-crystalline compound A is obtained by treating the aqueous solution containing the compound A and the citric acid with calcium carbonate, sulfuric acid, an organic solvent, etc. to remove the citric acid and the crystalline compound A in the solution. The three-dimensional structure of the crystalline compound A is an SS stereoisomer according to the R-S system. The three-dimensional structure of the non-crystalline compound A is an SR stereoisomer according to the R-S system.
(FR) La présente invention concerne un composé cristallin A obtenu par élimination de l'acide citrique dans une solution aqueuse. La dite solution aqueuse contenant un un composé A représenté par la formule (A) et de l'acide citrique est soumise à une chromatographie sur colonne échangeuse d'ions, ou à un traitement avec du carbonate de calcium. Le composé cristallin A est ainsi obtenu en soumettant ensuite ladite solution aqueuse à plusieurs étapes. La présente invention concerne également un composé non cristallin de haute pureté A qui est obtenu par traitement de la solution aqueuse contenant le composé A et de l'acide citrique avec du carbonate de calcium, de l'acide sulfurique, un solvant organique, etc., pour éliminer l'acide citrique et le composé cristallin A dans la solution. La structure tridimensionnelle du composé cristallin A est celle d'un stéréoisomère SS selon le système R-S. La structure tridimensionnelle du composé non cristallin A est celle d'un stéréoisomère SR selon le système R-S.
(JA) 下記式で示される化合物A及びクエン酸を含む水溶液に対してイオン交換カラムクロマトグラフィーまたは炭酸カルシウムを用いることによって、上記水溶液中のクエン酸を除去し、その後いくつかの工程を経て結晶性化合物Aを得る。また、高純度の非結晶性化合物Aは、化合物A及びクエン酸を含む水溶液に対して炭酸カルシウム、硫酸、有機溶媒等を用いて溶液中のクエン酸及び結晶性化合物Aを除去することによって得られる。結晶性化合物Aの立体構造はRS表示法でSS体である。非結晶性化合物Aの立体構造はRS表示法でSR体である。
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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)