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1. (WO2017148416) METHOD FOR PREPARING MAYTANSINE ESTERS AND INTERMEDIATE THEREOF
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Pub. No.: WO/2017/148416 International Application No.: PCT/CN2017/075448
Publication Date: 08.09.2017 International Filing Date: 02.03.2017
IPC:
C07D 498/18 (2006.01) ,C07D 249/18 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
498
Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
12
in which the condensed system contains three hetero rings
18
Bridged systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
249
Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
16
condensed with carbocyclic rings or ring systems
18
Benzotriazoles
Applicants:
凯惠科技发展(上海)有限公司 XDCEXPLORER (SHANGHAI) CO., LTD. [CN/CN]; 中国上海市 浦东新区张江高科技园区蔡伦路720弄3号楼302室 Room 302, No.3 Building, Lane 720 Cailun Road Zhangjiang High-Tech Park, Pudong New Area Shanghai 201203, CN
Inventors:
向少云 XIANG, Shaoyun; CN
杨鸿裕 YANG, Hongyu; CN
朱华萍 ZHU, Huaping; CN
马兴泉 MA, Xingquan; CN
Agent:
上海弼兴律师事务所 SHANGHAI BESHINING LAW OFFICE; 中国上海市 小木桥路681号外经大厦21楼 21st Floor, SFECO Mansion No.681 Xiaomuqiao Road Shanghai 200032, CN
Priority Data:
201610119508.203.03.2016CN
Title (EN) METHOD FOR PREPARING MAYTANSINE ESTERS AND INTERMEDIATE THEREOF
(FR) PROCÉDÉ DE PRÉPARATION D'ESTERS DE MAYTANSINE ET DE LEUR INTERMÉDIAIRE
(ZH) 一种美登素酯的制备方法及其中间体
Abstract:
(EN) Disclosed are a method for preparing maytansine esters as shown by formula (I) and an intermediate thereof. The method comprises a step of carrying out an interesterification reaction of compound (Ia) and RCOOR' in the presence of an organic solvent and a base to obtain the compound. The preparation method is mild in reaction conditions, easy in terms of synthesis and post-treatment steps, and high in reaction conversion and yield. Racemization phenomenon is not observed during the reaction, the product purity is high, the production cost is low, and the preparation method is suitable for industrial production. Reaction (1)
(FR) L'invention concerne un procédé de préparation d'esters de maytansine de formule I et d'un intermédiaire de ces derniers. Le procédé comprend une étape de mise en œuvre d'une réaction d'interestérification du composé Ia et de RCOOR' en présence d'un solvant organique et d'une base pour obtenir le composé. Le procédé de préparation présente des conditions de réaction douces, des étapes de synthèse et de post-traitement faciles, et une conversion et un rendement de réaction élevés. Le phénomène de racémisation n'est pas observé pendant la réaction, la pureté du produit est élevée, le coût de production est faible, et le procédé de préparation est approprié pour une production industrielle. Réaction (1)
(ZH) 一种式(I)所示美登素酯的制备方法及其中间体,所述方法包括在有机溶剂和碱存在下,将化合物(Ia)与RCOOR'进行酯交换反应得到所述化合物的步骤。该制备方法反应条件温和,合成及后处理步骤简单,反应转化率及产率高,反应过程中未观察到消旋现象,产品纯度高,生产成本低,适合于工业化生产。
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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, 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)