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F-BPA preparation method

A technology of F-BPA and compound, applied in the field of preparation of F-BPA, to achieve the effect of less impurities

Inactive Publication Date: 2018-07-20
NEUBORON MEDTECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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but little about 19 Report on the preparation method of F-BPA

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Embodiment 1

[0027] The preparation method of F-BPA

[0028] At room temperature, mix 325mL of dioxane and 325mL of water to form a reaction solvent, add 64.83g of 4-bromo-2-fluoro-phenylalanine to the reaction solvent, and then add 24.74g of sodium hydroxide and 91.78g of di-tert-butyl dicarbonate (Boc 2 O) The reaction was stirred for 16 h to obtain a mixture containing compound A.

[0029] The mixture was concentrated under reduced pressure, adjusted to pH 2-3 with hydrochloric acid, extracted with 650mL*3 ethyl acetate, the organic phase was washed with saturated brine, the separated organic phase was dried with anhydrous sodium sulfate and filtered, and the filtrate was again The compound A (80 g, yield 87.7%) was obtained by concentration under reduced pressure.

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Abstract

The invention discloses a new F-BPA preparation method, wherein F-BPA is prepared from 4-bromo-2-fluoro-phenylalanine. According to the present invention, the steps of the preparation method are simple, and the produced impurities are less, such that the more separation and purification steps are not required so as to reduce the production cost of F-BPA.

Description

technical field [0001] The invention relates to a preparation method of a compound, especially a preparation method of F-BPA. Background technique [0002] Boron neutron capture therapy (BNCT) treatment technology is an advanced dual-targeted tumor radiotherapy technology. This method is to give tumor patients a boron-containing drug that can be enriched in cancer cells in advance, and then irradiate the tumor area enriched with boron-containing drugs with neutrons, and use boron-10 isotopes to undergo nuclear reactions with neutrons to produce high-energy particles. The characteristic of selectively killing cancer cells without harming normal cells can effectively treat tumors. 4-Dihydroxyboryl-L-phenylalanine (BPA) is currently the most important boron-containing amino acid compound in BNCT drug development and clinical trials, and it can selectively accumulate in tumor cells. [0003] According to the properties of BPA that can penetrate the blood-brain barrier and accu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F5/02
Inventor 刘渊豪李世红何静
Owner NEUBORON MEDTECH
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