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Compounds, conjugates, kits and their use in the detection of estradiol

A technology of compounds and conjugates, which is applied in the field of analysis, can solve problems such as estradiol derivatives to be developed, and achieve the effect of being easy to popularize, apply and obtain

Active Publication Date: 2020-09-15
SHENZHEN MINDRAY BIO MEDICAL ELECTRONICS CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, currently applicable estradiol derivatives are still to be developed

Method used

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  • Compounds, conjugates, kits and their use in the detection of estradiol
  • Compounds, conjugates, kits and their use in the detection of estradiol
  • Compounds, conjugates, kits and their use in the detection of estradiol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] In this embodiment, compound shown in formula (2) is synthesized according to the following process:

[0059]

[0060] The synthetic route is as follows:

[0061]

[0062] Concrete synthetic steps are as follows:

[0063] 1. Synthesis of compound 2:

[0064] Feed 2.72g (0.01mol) of 17β-estradiol (compound 1) into a 100mL dry and cooled reaction flask, add 40mL of dimethylformamide (DMF), stir to dissolve, then add 3.14g (0.03mol) of anhydrous potassium carbonate , Under stirring, 2.17g (0.012mol) methyl 4-bromobutyrate was slowly added dropwise. After the dropwise addition was completed, the reaction was carried out for 4 hours. The reaction solution was poured into ice water, extracted three times with ethyl acetate, the combined organic layers were washed three times with saturated brine, then dried over anhydrous sodium sulfate and concentrated to obtain 4.7 g of crude compound 2.

[0065] MS: positive ion peak: 373.6, 395.6 (+Na peak); negative ion peak: 3...

Embodiment 2

[0070] In this embodiment, compound shown in formula (3) is synthesized according to the following process:

[0071]

[0072] The synthetic route is as follows:

[0073]

[0074] Concrete synthetic steps are as follows:

[0075] 1. Synthesis of compound 5:

[0076] Feed 2.70g (0.01mol) of estrone (compound 4) in a 100mL dry and cooled reaction flask, add 40mL of DMF, stir to dissolve, then add 3.14g (0.03mol) of anhydrous potassium carbonate, and slowly add 2.17g ( 0.012mol) methyl 4-bromobutyrate. After the dropwise addition was completed, the reaction was carried out for 4 hours. The reaction solution was poured into ice water, extracted three times with ethyl acetate, the combined organic layers were washed three times with saturated brine, then dried over anhydrous sodium sulfate and concentrated to obtain 4.6 g of crude compound 5.

[0077] MS: positive ion peak: 371.5, 393.5 (+Na peak); negative ion peak: 369.5.

[0078] 2. Synthetic formula (3) compound:

[...

Embodiment 3

[0082] In this embodiment, compound shown in formula (4) is synthesized according to the following process:

[0083]

[0084] synthetic route

[0085]

[0086] Concrete synthetic steps are as follows:

[0087] 1. Synthesis of compound 8:

[0088] Feed 2.88g (0.01mol) of estriol (compound 7) in a 100mL dry and cooled reaction flask, add 40mL of DMF, stir to dissolve, add 3.14g (0.03mol) of anhydrous potassium carbonate, and slowly add 2.17g (0.012 mol) methyl 4-bromobutyrate. After the dropwise addition was completed, the reaction was carried out for 4 hours. The reaction solution was poured into ice water, extracted three times with ethyl acetate, the organic layers were combined, washed three times with saturated brine, dried over anhydrous sodium sulfate, and concentrated to obtain 4.9 g of crude compound 8.

[0089] MS: positive ion peak: 389.7, 411.7 (+Na peak); negative ion peak: 387.8.

[0090] 2. Synthetic formula (4) compound:

[0091] Feed 4.9 g of the cru...

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Abstract

The invention discloses a compound, a conjugate, a kit for detecting estradiol and the use of the kit for detecting estradiol in detecting estradiol. The compound has a structure shown in formula (1), wherein, L represents the connecting arm, R 1 , R 2 , R 3 and R 4 are independently hydrogen, hydroxyl, C 1~3 Alkyl, C 1~3 Alkoxy, C 2~3 Alkenyl or C 2~3 Alkynyl. The compounds of the present invention can accurately detect estradiol.

Description

technical field [0001] The present invention relates to the field of analysis. In particular, the present invention relates to compounds, conjugates, kits and their use in the detection of estradiol. More specifically, the present invention relates to a compound, a conjugate, a kit for detecting estradiol and the use of the kit for detecting estradiol in detecting estradiol. Background technique [0002] Estrol refers to substances with the following core structural units, common ones are estrone, estradiol and estriol. [0003] [0004] At present, the principle of using immunological methods to detect estradiol is: since there is no functional group on estradiol that can be directly connected to the labeled molecule, it is necessary to introduce a structure that can be directly connected to the labeled molecule through chemical synthesis (called a connecting arm, and the terminal functional group can be is carboxyl, amino, etc.) to obtain estradiol derivatives. Next,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J1/00C12N9/08C12N9/16C12N9/48G01N33/74G01N33/68G01N33/535C12Q1/42C12Q1/37C12Q1/28
CPCC07J1/0059C07J1/0062C07J1/007C12N9/0065C12N9/16C12N9/48C12Q1/28C12Q1/37C12Q1/42C12Y111/01007C12Y301/03001G01N33/535G01N33/6854G01N33/743
Inventor 唐涛张裕平何飞
Owner SHENZHEN MINDRAY BIO MEDICAL ELECTRONICS CO LTD