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1. (WO2017096772) METHOD FOR PREPARING ANTI-HEART-FAILURE MEDICINE LCZ696
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/096772 International Application No.: PCT/CN2016/084914
Publication Date: 15.06.2017 International Filing Date: 06.06.2016
IPC:
C07D 257/04 (2006.01) ,C07C 233/47 (2006.01) ,C07C 231/02 (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
02
from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
Applicants:
浙江天宇药业股份有限公司 ZHEJIANG TIANYU PHARMACEUTICAL CO., LTD. [CN/CN]; 中国浙江省台州市 黄岩江口化工开发区 Huangyan Jiangkou Development Zone Taizhou, Zhejiang 318020, CN
Inventors:
朱国荣 ZHU, Guorong; CN
屠勇军 TU, Yongjun; CN
谢文龙 XIE, Wenlong; CN
王臻 WANG, Zhen; CN
徐少军 XU, Shaojun; CN
Agent:
国浩律师(上海)事务所 GRANDALL LAW FIRM (SHANGHAI); 中国上海市 静安区北京西路968号嘉地中心23楼 23/F, Garden Square, No.968 West Beijing Road, Jingan District Shanghai 200041, CN
Priority Data:
201510903519.509.12.2015CN
Title (EN) METHOD FOR PREPARING ANTI-HEART-FAILURE MEDICINE LCZ696
(FR) PROCÉDÉ DE PRÉPARATION DE MÉDICAMENTS LCZ696 CONTRE L'INSUFFISANCE CARDIAQUE
(ZH) 一种抗心衰药LCZ696的制备方法
Abstract:
(EN) Disclosed is a method for preparing an anti-heart-failure medicine LCZ696. The preparing method comprises the following steps (formula (I)): in an organic solvent, a sacubitril dicyclohexylamine salt reacts with valsartan under the effect of a sodium hydroxide aqueous solution, and the anti-heart-failure medicine LCZ696 is obtained. The preparing method of the present invention is simple in process and omits the procedures of ion exchange from a sodium salt to a calcium salt and hydrochloric acid dissociation in an existing production process, residues of calcium ions are avoided, and the production efficiency is effectively improved.
(FR) L'invention concerne un procédé de préparation d'un médicament LCZ696 contre l'insuffisance cardiaque. Le procédé de préparation comprend les étapes suivantes (formule (I)) : la réaction, dans un solvant organique, d'un sel de dicyclohexylamine de sacubitril avec du valsartan sous l'effet d'une solution aqueuse d'hydroxyde de sodium et l'obtention du médicament LCZ696 contre l'insuffisance cardiaque. Le processus du procédé de préparation selon la présente invention est simple et élimine les procédés d'échange d'ions d'un sel de sodium à un sel de calcium et la dissociation d'acide chlorhydrique d'un processus de préparation existant, des résidus d'ions calcium sont évités et le rendement de production est efficacement amélioré.
(ZH) 本发明公开了一种抗心衰药LCZ696的制备方法。该制备方法包括下述步骤(式(I)):有机溶剂中,在氢氧化钠水溶液的作用下,沙库比曲二环己胺盐与缬沙坦反应,即可。本发明的制备方法工艺简单,省去现有的生产工艺中的钠盐到钙盐的离子交换和盐酸游离的工序,且不存在钙离子残留,有效提高生产效率。
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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, 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, 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:
EP3388424US20180354915