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1. (WO2017097193) METHOD FOR REFINING LISINOPRIL HYDRIDE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/097193 International Application No.: PCT/CN2016/108814
Publication Date: 15.06.2017 International Filing Date: 07.12.2016
IPC:
C07C 233/47 (2006.01) ,C07C 231/24 (2006.01) ,C07K 5/068 (2006.01) ,A61P 9/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
233
Carboxylic acid amides
01
having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
45
having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
46
with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
47
having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
231
Preparation of carboxylic acid amides
22
Separation; Purification; Stabilisation; Use of additives
24
Separation; Purification
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
5
Peptides having up to four amino acids in a fully defined sequence; Derivatives thereof
04
containing only normal peptide links
06
Dipeptides
068
the side chain of the first amino acid containing more amino groups than carboxyl groups, or derivatives thereof, e.g. Lys, Arg
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9
Drugs for disorders of the cardiovascular system
12
Antihypertensives
Applicants:
浙江华海药业股份有限公司 ZHEJIANG HUAHAI PHARMACEUTICALS CO., LTD. [CN/CN]; 中国浙江省 临海汛桥 Xunqiao, Linhai Zhejiang 317024, CN
Inventors:
胡佳兴 HU, Jiaxing; CN
黄文锋 HUANG, Wenfeng; CN
涂国良 TU, Guoliang; CN
林恩敏 LIN, Enmin; CN
王安宇 WANG, Anyu; CN
方玉玲 FANG, Yuling; CN
Agent:
北京邦信阳专利商标代理有限公司 BOSS&YOUNG PATENT AND TRADEMARK LAW OFFICE; 中国北京市 朝阳区建国门外大街永安东里甲3号通用时代国际中心A座5层 5/F., Tower A, GT International Center, Jia 3 Yongandongli, Jianguomenwai Ave., ChaoyangDistrict, Beijing 100022, CN
Priority Data:
201510920150.911.12.2015CN
Title (EN) METHOD FOR REFINING LISINOPRIL HYDRIDE
(FR) PROCÉDÉ DE RAFFINAGE D'HYDRURE DE LISINOPRIL
(ZH) 一种赖诺普利氢化物的精制方法
Abstract:
(EN) The present invention provides a method for refining a lisinopril hydride crude product by means of solvent crystallization. The method specifically comprises: adding ketones solvents into a crude product which contains lisinopril hydride (I), lisinopril isomer (II) and other impurities (such as impurities III, IV), dissolving by heating, cooling for crystallizing for the first time, selectively adding seed crystal, then cooling for crystallizing, culturing crystal, continuously cooling for crystallizing, and carrying out suction filtration to obtain the lisinopril hydride, the yield reaching 80%, and the purity reaching up to 97% or more and even reaching up to 98% or more. The method can separate and refine hydride in a lisinopril hydride crude product, and increases the refining yield of lisinopril hydride, thereby having obvious utilization value in industrial application.
(FR) La présente invention concerne un procédé de raffinage d'un produit brut d'hydrure de lisinopril par cristallisation par solvant. Le procédé comprend précisément : l'ajout de solvants de type cétone dans un produit brut qui contient de l'hydrure de lisinopril (I), de l'isomère de lisinopril (II) et d'autres impuretés (telles que des impuretés III, IV), la dissolution par chauffage, le refroidissement pour une première cristallisation, l'ajout sélectivement de germe cristallin, puis le refroidissement pour la cristallisation, la culture du cristal, le refroidissement continu pour la cristallisation et la conduite d'une filtration par aspiration, pour obtenir l'hydrure de lisinopril, le rendement atteignant 80 %, et la pureté atteignant jusqu'à 97 % ou plus et atteignant même jusqu'à 98 % ou plus. Le procédé peut séparer et raffiner l'hydrure en un produit brut d'hydrure de lisinopril, et augmenter le rendement de raffinage de l'hydrure de lisinopril, ayant de là une valeur d'utilisation évidente dans une application industrielle.
(ZH) 本发明提供了一种通过溶剂结晶,对赖诺普利氢化物粗品进行精制的方法,具体为利用将含有赖诺普利氢化物(Ι)、赖诺普利异构体(II)以及其它杂质(如杂质III、IV)的粗品加入酮类溶剂,加热溶解,首次降温析晶,选择性地加入晶种接着降温析晶,养晶、继续降温析晶,抽滤即可得到赖诺普利氢化物,收率达80%,纯度达97%以上,更能达98%以上。该方法可将赖诺普利氢化物粗品中的氢化物进行分离精制,提高赖诺普利氢化物精制产率,在工业应用上具有明显的利用价值。
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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, JP, KE, KG, 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 Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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: Chinese (ZH)
Filing Language: Chinese (ZH)