Technetium-labeled estradiol derivative and reference compound thereof, and preparation method, application and intermediate thereof

A compound, the technology of estradiol, which is applied in the field of technetium-labeled estradiol derivatives and their reference compounds, can solve the problems of poor imaging effect, poor target tissue selectivity, and high lipophilicity
CN102030797BInactive Publication Date: 2013-03-20SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGHAI INST OF APPLIED PHYSICS - CHINESE ACAD OF SCI
Publication Date
2013-03-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a technetium-labeled estradiol derivative and a reference compound thereof, and a preparation method, an application and an intermediate thereof. The technetium-labeled estradiol derivative is shown in the formula VII, wherein A is a group -(CH2CH2)x- or -(CH2CH2O)m(CH2CH2)n-; and x, m and n are integral numbers, x is 1-6, m is 1-3, and n is 1-3. The technetium-labeled estradiol derivative has a moderate lipid / water partition coefficient, and can be used for preparing imaging drugs for diagnosing breast cancer. The in-vitro experiment indicates that the technetium-labeled estradiol derivative has favorable affinity with an estrogen receptor, and has favorable in-vitro stability and moderate metabolism speed in phosphate buffer solution (PBS), 1mM histidine solution, 1mM cysteine solution, 1mM diethylene triamine pentacetic acid (DTPA) solution and newborn calf serum. The technetium-labeled estradiol derivative is hopeful to become a radioactive drug which has good targeting property, is suitable for continuing deep research in organisms and is used for diagnostic imaging.
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Description

technical field

[0001] The invention relates to a technetium-labeled estradiol derivative and its reference compound, its preparation method, application and its intermediate. Background technique

[0002] Nuclear medicine can use the special physical properties of labeled nuclides in certain radiopharmaceuticals to image a variety of tumors and their lesions. This unique method of tumor diagnosis has been paid more and more attention in clinic. Currently, radionuclides used for imaging mainly include 131 I. 153 Sm, 117 mSn, 186 Re, 188 Re and 99m Tc et al. in, 99m Tc has attracted much attention in the field of tumor diagnosis because of its excellent physical and chemical properties. 99m The half-life of Tc is 6.02 hours, the energy of gamma rays is 140keV, the radiation damage is small, and it has good imaging resolution, and it can be easily obtained from 99 Mo- 99m Tc generator rinses to get Na 99m TCO 4 solution. Because of its cheap and easy to obtain, l...

Claims

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