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1. CN109705104 - Preparation method and application for gadolinium ion type contrast agent intermediate

Office
Chine
Numéro de la demande 201910078991.8
Date de la demande 28.01.2019
Numéro de publication 109705104
Date de publication 03.05.2019
Numéro de délivrance 109705104
Date de délivrance 26.05.2020
Type de publication B
CIB
C07D 405/04
CCHIMIE; MÉTALLURGIE
07CHIMIE ORGANIQUE
DCOMPOSÉS HÉTÉROCYCLIQUES
405Composés hétérocycliques contenant à la fois un ou plusieurs hétérocycles comportant des atomes d'oxygène comme uniques hétéro-atomes du cycle et un ou plusieurs hétérocycles comportant des atomes d'azote comme uniques hétéro-atomes du cycle
02contenant deux hétérocycles
04liés par une liaison directe de chaînon cyclique à chaînon cyclique
C07D 257/02
CCHIMIE; MÉTALLURGIE
07CHIMIE ORGANIQUE
DCOMPOSÉS HÉTÉROCYCLIQUES
257Composés hétérocycliques contenant des cycles comportant quatre atomes d'azote comme uniques hétéro-atomes du cycle
02non condensés avec d'autres cycles
CPC
A61K 49/106
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
08characterised by the carrier
10Organic compounds
101the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
106the complex-forming compound being cyclic, e.g. DOTA
C07D 257/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
257Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
02not condensed with other rings
C07D 405/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
405Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02containing two hetero rings
04directly linked by a ring-member-to-ring-member bond
A61K 49/108
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
49Preparations for testing in vivo
06Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
08characterised by the carrier
10Organic compounds
101the carrier being a complex-forming compound able to form MRI-active complexes with paramagnetic metals
106the complex-forming compound being cyclic, e.g. DOTA
108the metal complex being Gd-DOTA
Déposants HUBEI TIANSHU PHARMACEUTICAL CO., LTD.
湖北天舒药业有限公司
Inventeurs ZHANG ZHIHUA
张志华
LIU YUNLONG
刘云龙
Mandataires 北京路浩知识产权代理有限公司 11002
北京路浩知识产权代理有限公司 11002
Titre
(EN) Preparation method and application for gadolinium ion type contrast agent intermediate
(ZH) 钆系离子型造影剂中间体的制备方法及其应用
Abrégé
(EN) The invention provides a preparation method and an application for a gadolinium ion type contrast agent intermediate. The preparation method comprises the following steps: allowing a substance as shown in a general formula (II) which is described in the specification to react with a substance as shown in a general formula (III) which is described in the specification or a substance as shown in a general formula (IV) which is described in the specification in the presence of an alkaline catalyst so as to generate the gadolinium ion type contrast agent intermediate with a structure as shown in ageneral formula (I) or a general formula (V) which are described in the specification. In the general formulas as described in the specification, R represents a group selected from the group consisting of C1-C5 alkyl groups, benzyl groups and benzyl derivatives; R1 represents -H or -CH2OH; and R2 represents -CH3 or -OH. The above-mentioned preparation method used to prepare the gadolinium ion type contrast agent intermediate with a structure as shown in the general formula (I) which is described in the specification has the advantages of simple reaction, fewer steps and controllable reaction,and can reach a yield of 99% or above; and a product obtained by using the preparation method provided by the invention has a purity of more than 99.5%.
(ZH) 本发明提供了一种钆系离子型造影剂中间体的制备方法及应用。该制备方法包括如下步骤:通式(II)所示的物质和通式(III)所示的物质或通式(IV)所示的物质在碱性催化剂存在下,反应生成含有通式(I)或通式(V)所示结构的钆系离子型造影剂中间体;其中,R代表C1‑C5的烷基、苄基或苄基衍伸物,R1代表‑H或‑CH2OH,R2代表‑CH3或‑OH。使用上述制备方法制备含有通式(I)所示结构的钆系离子型造影剂中间体,反应简单,步骤少,反应可控,产率可达99%及以上,得到的产物的纯度大于99.5%。
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EP2019908100This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.