A radionuclide-labeled estrogen receptor molecular targeting compound and its application
A technology of estrogen receptors and radionuclides, which is applied in the field of estrogen receptor molecular targeting compounds, can solve the problems of non-specific uptake and unsatisfactory uptake of radiotracers, and achieve improved imaging contrast and good metabolic stability in the body Sexuality, the effect of increasing the ratio
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Embodiment 1
[0055] Synthesis of compound 4-1: when R in the above structural formula 1 to R 5 = H, R 6 = 131 I (radioactive iodine isotope), R 7 = 127 When I and n=0, it is compound 4-1. The radioactive iodine isotope is labeled by "click" chemical reaction, and its synthetic route and preparation method are as follows:
[0056]
[0057] Specifically include the following steps:
[0058] 1) Synthesis of 3-azidopropylamine:
[0059] 3-Bromopropylamine hydrochloride (5 g, 38 mmol) was dissolved in 20 mL of deionized water at room temperature. At 0°C, an aqueous solution of sodium azide (7.5 g, 115 mmol, 20 mL) was added dropwise to the above solution. After the dropwise addition, the temperature was raised to 80° C., and the reaction was carried out overnight. The reaction system was cooled to 0°C, and 50 mL of diethyl ether was added. Weigh 4g of potassium hydroxide particles and slowly add to the reaction flask, keeping the low temperature. Extracted with diethyl ether (50 m...
Embodiment 2
[0065] Synthesis of compound 4-2: when R in the above structural formula 1 = H, R 2 = F, R 3 , R 4 = H, R 5 =OCH 3 , R 6 = 131 I (radioactive iodine isotope), R 7 = 127 When I and n=0, it is compound 4-2. The radioactive iodine isotope is labeled by "click" chemical reaction, and its synthetic route and preparation method are as follows:
[0066]
[0067] 1) Synthesis of 4-fluoro-17α-alkynyl-11β-methoxyestradiol:
[0068] Under a nitrogen atmosphere, N-fluoropyridinium triflate (1.83 g, 7.4 mmol) was added to 17α-alkynyl-11β-methoxyl in 16 mL of 1,1,2-trichloroethane estradiol (1.2g, 3.7mmol). After the reaction was complete, the solvent was removed by rotary evaporation, and the residue was poured into water and extracted with dichloromethane. The crude product was purified by column chromatography (ethyl acetate / dichloromethane=1:9) to obtain 0.8 g of light yellow solid with a yield of 63%.
[0069] 2) Labeling of compound 4-2:
[0070] Add 4 mL of anhydrous...
Embodiment 3
[0072] Synthesis of compound 8-1: when R in the above structural formula 1 , R 2 , R 3 , R 4 , R 5 and R 6 = H, and R 7 = 125 I (radioactive iodine isotope), when n=3, it is compound 8-1. The radioactive iodine isotope is labeled with phenylboronic acid precursor, and then connected to the estrogen structure. The synthetic route and preparation method are as follows:
[0073]
[0074] Specifically include the following steps:
[0075] 1) Synthesis of (2-(2-(2-(2-(2-azidoethoxy) ethoxy) ethoxy) ethyl) tert-butyl carbamate:
[0076] 2-(2-(2-(2-(2-Azidoethoxy)ethoxy)ethoxy)ethylamine (1 g, 4.6 mmol) and triethylamine (0.7 g, 6.9 mmol) were mixed with Anhydrous 5mL tetrahydrofuran was dissolved and stirred at room temperature for 0.5h. Di-tert-butyl dicarbonate (1.1g, 5mmol) was added and reacted overnight at room temperature. The reaction solvent was spin-dried and extracted with ethyl acetate (40mL×3). The organic layer was collected and The solvent was removed, and...
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