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Diphosphonic acid derivative, radioactive 99mTc labeled diphosphonic acid derivative and uses thereof

A kind of derivative, bisphosphonic acid technology, applied in the field of bisphosphonic acid derivatives, can solve the problems such as not being satisfied

Active Publication Date: 2005-06-01
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to obtain markers of a single structure, it was used 123 I labeled bisphosphonates, but did not get satisfactory results

Method used

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  • Diphosphonic acid derivative, radioactive 99mTc labeled diphosphonic acid derivative and uses thereof
  • Diphosphonic acid derivative, radioactive 99mTc labeled diphosphonic acid derivative and uses thereof
  • Diphosphonic acid derivative, radioactive 99mTc labeled diphosphonic acid derivative and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Embodiment 1: Synthesis of HYNIC-AMDP

[0111] The synthesis of HYNIC-AMDP is carried out according to the following reaction scheme 1':

[0112] Reaction Scheme 1'

[0113]

[0114] [1] Add 80% hydrazine hydrate (8.8mL, 232.5mmol) and compound 1 (2.0g, 12.7mmol) into a 25mL single-necked bottle equipped with a reflux condenser, heat in an oil bath at 100°C for 4h, then cool to room temperature , concentrated and dissolved in water, adjusted to pH 5.5 with concentrated hydrochloric acid, filtered, the obtained solid was washed with 95% ethanol and ether, and dried in vacuo to obtain 1.5 g of compound 2 with a yield of 77%. θm.p.291~293℃.

[0115] 1 HNMR (D 2 O) δ: 8.01 (s, 1H), 7.91 (d, 1H), 6.67 (d, 1H).

[0116] [2] Boc (2.13g, 9.8mmol) was added to a DMF (10mL) solution of compound 2 (1.4g, 9.8mmol) and triethylamine (1.2mL, 11.8mmol), and the reaction mixture became homogeneous after 1h , Continue to stir at room temperature for 16h, remove the precipitate ...

Embodiment 2

[0122] Embodiment 2: the synthesis of DMP-AMDP

[0123] The synthesis of DMP-AMDP is carried out according to the following reaction scheme 2':

[0124] Reaction scheme 2'

[0125]

[0126] [1] Dissolve 2,3-dibromopropionic acid (9.56g, 40mmol) white solid powder in 50mL1mol L under ice bath -1 in KOH solution (solution 1); measure 9mL (9.32g, 120mmol) of thioacetic acid light yellow irritating liquid, dissolve in 120mL1mol L under ice bath -1 In the KOH solution (solution 2), the solution 1 was slowly dropped into the solution 2, and reacted in a 250mL three-necked flask at room temperature for 24h, and nitrogen was protected during the reaction. The reaction solution was acidified with concentrated hydrochloric acid to pH 3, extracted with ethyl acetate, the light yellow organic phase was dried with anhydrous magnesium sulfate, placed in the refrigerator overnight, the desiccant was removed by suction filtration, and 7.2 g of compound 6 was obtained by removing the solv...

Embodiment 3

[0133] Embodiment 3: Synthesis of HYNIC-ACPDP

[0134] The synthesis of HYNIC-ACPDP is carried out according to the following reaction scheme 3':

[0135] Reaction scheme 3'

[0136]

[0137] [1] Add compound 3 (0.33g, 1.3mmol), 1-hydroxybenzotriazole (HOBt, 0.18g, 1.3mmol) and compound 9 (0.40g, 1mmol) in a 50mL three-necked flask, according to the literature Georges Sturtz, et al., Synthesis, 1991: 661 ~ 662 method synthesis) dissolved in 10mL N, N-dimethylformamide (DMF), cooled to 0 ° C in an ice bath, added dicyclohexylcarbodiimide ( DCC, 0.27g, 1.3mmol), continued to stir at room temperature overnight, filtered, the filtrate was concentrated under reduced pressure, and separated and purified by silica gel column to obtain 0.31g of compound 10 with a yield of 48%.

[0138] 1 HNMR (CDCl 3 )δ: 8.64(s, 1H), 8.03(s, 1H), 7.88~7.70(m, 1H), 7.44~7.35(m, 1H), 6.77(d, 1H), 4.75(m, 1H, P- CH-P), 4.24~4.20(m, 11H, 4×OCH 2 CH 3 , COOCH 2 CH 3 , CHCOOC 2 h 5 ), 1.45(m, ...

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Abstract

The present invention relates to diphosphonic acid derivative, and 99mTc labeled diphosphonic acid derivative ligand or the label obtained through labeling diphosphonic acid derivative ligand and coligand. The label may be used in preparing developer for human and animal organs, especially bone.

Description

technical field [0001] The present invention relates to a new class of bisphosphonic acid derivatives, in particular to bisphosphonic acid derivatives with bifunctional linkers introduced into their structures. The invention also relates to the use of 99m Part of the diphosphonic acid derivatives labeled with Tc, or the markers obtained by marking part of the diphosphonic acid derivatives and their co-ligands, and the markers are used in the preparation of imaging agents for human and animal organs or tissues, especially Use in the preparation of bone imaging agents. Background technique [0002] Radionuclide bone imaging is one of the advantages of nuclear medicine diagnosis. In the nuclear medicine departments of developed countries such as the United States, Britain, and Japan, bone imaging accounts for more than half of the total workload. my country's bone imaging work is also increasing year by year. [0003] Bone scintigraphy is widely used in the diagnosis of met...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/00C07F9/38C07F9/58
Inventor 王学斌刘丽琴陆洁唐志刚张现忠
Owner BEIJING NORMAL UNIVERSITY
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