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1. (WO2018205402) SYNTHETIC METHOD FOR ULARITIDE
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Pub. No.: WO/2018/205402 International Application No.: PCT/CN2017/092715
Publication Date: 15.11.2018 International Filing Date: 13.07.2017
IPC:
C07K 14/58 (2006.01) ,C07K 1/20 (2006.01) ,C07K 1/06 (2006.01) ,C07K 1/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
14
Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
435
from animals; from humans
575
Hormones
58
Atrial natriuretic factor complex; Atriopeptin; Atrial natriuretic peptide (ANP); Cardionatrin; Cardiodilatin
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
14
Extraction; Separation; Purification
16
by chromatography
20
Partition-, reverse-phase or hydrophobic interaction chromatography
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
06
using protecting groups or activating agents
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
K
PEPTIDES
1
General processes for the preparation of peptides
04
on carriers
Applicants:
深圳翰宇药业股份有限公司 HYBIO PHARMACEUTICAL CO., LTD. [CN/CN]; 中国广东省深圳 南山区高新技术工业园中区翰宇生物医药园办公大楼四层 4th Floor, Hybio Medicine Park Office Building High-tech Industrial Park Central District, Nanshan Shenzhen, Guangdong 518057, CN
Inventors:
陈学明 CHEN, Xue Ming; CN
曾驰 ZENG, Chi; CN
宓鹏程 MI, Peng Cheng; CN
陶安进 TAO, An Jin; CN
袁建成 YUAN, Jian Cheng; CN
Agent:
北京市诚辉律师事务所 BEIJING CHENGHUI LAW FIRM; 中国北京市 朝阳区朝阳北路99号楼2单元905 905, Tower2, No. 99 Chaoyang North Road, Chaoyang District Beijing 100123, CN
Priority Data:
201710325145.210.05.2017CN
Title (EN) SYNTHETIC METHOD FOR ULARITIDE
(FR) PROCÉDÉ DE SYNTHÈSE DE L'ULARITIDE
(ZH) 一种乌拉立肽的合成方法
Abstract:
(EN) The present invention provides a preparation method for ularitide, comprising the following steps: 1) sequentially coupling Fmoc-AA-OH on a solid-phase synthetic resin; 2) removing the resin with a lysis buffer; and 3) reacting an intermediate obtained in step 2) with sodium thiosulfate pentahydrate in a solvent at the reaction temperature of 25-100°C, and completely reacting to obtain ularitide. The method of the present invention is appropriate to industrial preparation, and the yield thereof is greatly improved relative to the efficiency and yield of the solid-phase synthetic method.
(FR) La présente invention concerne un procédé de préparation de l'ularitide, comprenant les étapes suivantes : 1) couplage séquentiel Fmoc-AA-OH sur une résine synthétique en phase solide; 2) élimination de la résine avec un tampon de lyse; et 3) réaction d'un intermédiaire obtenu à l'étape 2) avec du pentahydrate de thiosulfate de sodium dans un solvant à la température de réaction de 25 à 100 °C, et la réaction complète pour obtenir de l'ularitide. Le procédé de la présente invention est approprié à une préparation industrielle, et le rendement de celui-ci est considérablement amélioré par rapport à l'efficacité et au rendement du procédé de synthèse en phase solide.
(ZH) 本发明提供了一种乌拉立肽的制备方法,其包括以下步骤:1)在固相合成树脂上,依次偶联Fmoc-AA-OH;2)裂解液脱除树脂;3)将步骤2)所得中间体与五水合硫代硫酸钠在溶剂中进行反应,反应温度为25-100℃,至反应完全得乌拉立肽。本发明的方法适合工业上制备,产率相比于固相合成方法效率和产率均有较高的提高。
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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: Chinese (ZH)
Filing Language: Chinese (ZH)