Scopoletin labeled by stable isotope and synthetic method for scopoletin

A stable isotope and isotope labeling technology, which is applied in the direction of isotope introduction of heterocyclic compounds, organic chemistry methods, organic chemistry, etc., can solve the problems of isotope-labeled scopoletin research and no reports, etc., and achieve high product yield and easy operation Effects that are easy to implement and synthesize with simple steps
CN105884733AActive Publication Date: 2016-08-24ZHENGZHOU TOBACCO RES INST OF CNTC +1
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHENGZHOU TOBACCO RES INST OF CNTC
Publication Date
2016-08-24

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Abstract

The invention belongs to the synthesis field of isotope labeled compound synthesis, and particularly relates to scopoletin labeled by stable isotope and a synthetic method for the scopoletin. The synthetic method is characterized in that scopoletin labeled acetylchloride-2-13 C is taken as a raw material, and the scopoletin labeled acetylchloride-2-13C reacts with 2,4-dihydroxyl-5-methoxybenzaldehyde to generate 2-aldehyde-4-methoxy-5-hydroxyl phenyl acetate; under the action of a basic catalyst, scopoletin-2-13C is generated through Perkin reaction. The synthetic method is simple in synthesis step, is gentle in reaction condition, is simple and convenient in operation, is high in product yield being 26% or higher, is capable of effectively synthesizing an isotope labeled coumarin derivative, so that a novel way is provided for synthesizing the isotope labeled coumarin derivative. Certain innovation and unique research significance are achieved on organic synthetic method.
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Description

technical field

[0001] The invention belongs to the field of isotope-labeled compound synthesis, in particular to a preparation of stable isotope-labeled scopolamine-2- 13 Synthesis of C. This compound is an important building block for the preparation of isotopically labeled coumarin derivatives. Background technique

[0002] Scopolamine belongs to the class of coumarin compounds, which is a kind of important organic heterocyclic compounds with benzopyrone as the parent structure modification. This type of compound is widely found in a variety of Chinese herbal medicines. Due to its special lactone structure, it has a wide range of pharmacological activities. In addition to its heat-clearing, analgesic, antibacterial and anti-inflammatory effects, it is used in some vascular diseases such as vasodilation and anticoagulation. It also has significant curative effect and certain anticancer activity.

[0003] Isotope-labeled compounds have important applications as tracer re...

Claims

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