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1. (WO2017097085) PREPARATION METHOD FOR EUTECTIC HYDRATE CRYSTAL FORM II OF AHU-377 AND DIOVAN TRISODIUM SALT
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/097085 International Application No.: PCT/CN2016/105335
Publication Date: 15.06.2017 International Filing Date: 10.11.2016
IPC:
C07D 257/04 (2006.01) ,C07C 233/47 (2006.01) ,C07C 231/24 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
257
Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02
not condensed with other rings
04
Five-membered rings
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
Applicants:
苏州晶云药物科技有限公司 CRYSTAL PHARMATECH CO., LTD. [CN/CN]; 中国江苏省苏州市 苏州工业园区星湖街218号生物纳米园B4-101 B4-101, Biobay, 218 Xinghu Street, Suzhou Industrial Park Suzhou, Jiangsu 215123, CN
Inventors:
陈敏华 CHEN, Minhua; CN
张炎锋 ZHANG, Yanfeng; CN
张良 ZHANG, Liang; CN
Agent:
苏州创元专利商标事务所有限公司 SUZHOU CREATOR PATENT & TREADMARK AGENCY LTD.; 中国江苏省苏州市 干将西路93号 No.93 Ganjiang West Road Suzhou, Jiangsu 215002, CN
Priority Data:
201510902127.708.12.2015CN
Title (EN) PREPARATION METHOD FOR EUTECTIC HYDRATE CRYSTAL FORM II OF AHU-377 AND DIOVAN TRISODIUM SALT
(FR) PROCÉDÉ DE PRÉPARATION D'UNE FORME CRISTALLINE II D'HYDRATE EUTECTIQUE D'UN SEL TRISODIQUE DU AHU-377 ET DU DIOVAN
(ZH) 一种AHU-377和缬沙坦三钠盐共晶水合物晶型II的制备方法
Abstract:
(EN) Disclosed is a preparation method for a eutectic hydrate crystal form II of AHU-377 and diovan trisodium salt, comprising: firstly, obtaining a clear solution of an AHU-377 and diovan trisodium salt compound, a solvent of the clear solution consisting of an anti-solvent and an n-solvent of a target product crystal form II, and the boiling point of the n-solvent being lower than that of the anti-solvent; secondly, removing the n-solvent and water from a system by evaporation under closed conditions; and finally, selectively adding a seed crystal of the crystal form II, and additionally adding a mixture of water and a carrier solvent to perform stirring crystallization. The method in the present invention can prepare a crystal form II, and has a stable and controllable technological process. The prepared crystal form II product is high in chemical purity, crystal form purity and fluidity, the process can be amplified, and demands for large-scale production are met.
(FR) L'invention concerne un procédé de préparation d'une forme cristalline II d'hydrate eutectique d'un sel trisodique du AHU-377 et du diovan, consistant à : tout d'abord obtenir une solution claire d'un composé de sel trisodique du AHU-377 et du diovan, un solvant de la solution claire consistant en un anti-solvant et un n-solvant d'une forme cristalline II du produit cible, et le point d'ébullition du n-solvant étant inférieur à celui de l'anti-solvant; ensuite éliminer le n-solvant et l'eau d'un système par évaporation dans des conditions fermées; et enfin ajouter sélectivement un germe cristallin de la forme cristalline II, et ajouter en outre un mélange d'eau et d'un solvant transporteur pour réaliser la cristallisation sous agitation. Dans la présente invention, ledit procédé peut préparer une forme cristalline II, et comprend un processus technologique stable et régulable. Ledit produit de forme cristalline II préparé présente des propriétés élevées de pureté chimique, de pureté et de fluidité de la forme cristalline, ledit procédé peut être amplifié, et les demandes de production à grande échelle sont satisfaites.
(ZH) 本发明公开了一种AHU-377和缬沙坦三钠盐共晶水合物晶型II的制备方法,首先获得AHU-377和缬沙坦三钠盐复合物的澄清溶液,该澄清溶液的溶剂由目标产物晶型II的反溶剂和正溶剂构成,且正溶剂的沸点低于反溶剂;其次,通过在密闭条件下蒸发除去体系中的正溶剂和水;最后,选择性地加入晶型II的晶种并补加水和载体溶剂的混合物,进行搅拌析晶。本发明的方法能够制备出晶型II,并且其工艺过程稳定可控,制备的晶型II产品化学纯度和晶型纯度高,流动性好,工艺可实现放大并满足规模化生产的需求。
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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)
Also published as:
CA3007864AU2016368863IL259871KR1020180090346EP3385256US20180354916
IN201817024422