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Coupling agent for preparing radiotherapy marker, 211At marker prepared thereby and preparation

A radiotherapy and 211at technology, which is applied in the field of 211At markers and coupling agents for their preparation, can solve the problems of difficult separation, low yield, complex reaction, etc., and achieve the effect of simple reaction, high yield and few reaction steps

Inactive Publication Date: 2011-10-26
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Borane isothiocyanate derivatives can be obtained by group modification with 2,3,5,6-tetrafluorophenol 3-(nested carborane) propionate (TCP), but the reaction is complicated and the yield low and difficult to separate

Method used

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  • Coupling agent for preparing radiotherapy marker, 211At marker prepared thereby and preparation
  • Coupling agent for preparing radiotherapy marker, 211At marker prepared thereby and preparation
  • Coupling agent for preparing radiotherapy marker, 211At marker prepared thereby and preparation

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Embodiment Construction

[0036] Below by embodiment the present invention will be further described. In the following examples, the mentioned component parts are parts by mass unless otherwise specified.

[0037] (1) Synthetic embodiment of TCP

[0038] The synthesis route of TCP is attached image 3 shown.

[0039] Weigh 2.0g (20.4mmol) of 4-pentynoic acid in a 150mL three-necked flask, dissolve it with 60mL of anhydrous THF, then add 6.45g (31mmol) DCC and 6.83g (41mmol) TFP to the flask, and the mixture It immediately turned pale yellow and produced a white precipitate. The mixture was stirred overnight at room temperature, then 0.1 mL of glacial acetic acid was added, and stirring was continued for 1 h. Filter, wash the precipitate with anhydrous THF, and distill the filtrate under reduced pressure on a rotary evaporator, dissolve the spin-dried product with 80 mL of n-hexane, remove the insoluble matter by filtration and wash the precipitate with 10 mL of n-hexane, and dissolve the filtrate i...

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Abstract

The invention discloses a coupling agent 2, 3, 5, 6-4-tetrafluorophenol 3-propionate TCP which can be used for preparing a radiotherapy marker, a radiotherapy marker <211>At-TCP-BSA which is prepared from the 2, 3, 5, 6-4-tetrafluorophenol 3-propionate TCP, as well as preparation methods of the coupling agent TCP and the marker <211>At-TCP-BSA. The marker <211>At-TCP-BSA prepared by the preparation method is used for radiotherapy, the marking rate can reach 60 percent, and the radiochemical purity is higher than 98 percent and has no significant change after the marker are placed at room temperature for 24 hours. Compared with free <211>At and <211>At-ATE-BSA (ATE is 3-n-butyltin N-succinimide benzoate), the marker <211>At-TCP-BSA has relatively high stability both in vivo and in vitro; and the TCP is a good intermediate for marking protein by radioactive astatine and lays a good function for the targeted cancer therapy of <211>At-TCP-BSA in the next stage.

Description

Technical field: [0001] The invention relates to the technical field of markers for radiotherapy of malignant tumors, in particular to 211 At markers and coupling agent technology for their preparation. Background technique: [0002] Carriers with high specificity and affinity for tumors, such as proteins, monoclonal antibodies, polypeptide ligands, and some compounds, are labeled with radionuclides to perform targeted radiation therapy on tumors in vivo, which is considered to be very promising. It has been paid more and more attention by various countries, and has made considerable clinical progress. Selecting an excellent targeting carrier and matching ideal nuclide is the primary problem in the research of nuclide-targeted therapy. The use of appropriate labeling methods to obtain radiopharmaceuticals that are stable in vivo and in vitro and maintain carrier-targeting properties is the basis and key of nuclide-targeted therapy research. [0003] More and more studies ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F5/02A61K51/08A61K51/10A61P35/00A61K101/02
Inventor 杨远友刘宁廖家莉
Owner SICHUAN UNIV