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A kind of 18f-pet/ct tracer with 7-deaza adenine base as mother nucleus and preparation method thereof
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A technology of 18F-HX and tracer, applied in organic chemical methods, chemical instruments and methods, preparations for in vivo tests, etc.
Active Publication Date: 2021-06-25
WEST CHINA HOSPITAL SICHUAN UNIV +1
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However, the types of tracers that can be used for the diagnosis of lung cancer are still very limited, so it is urgent to develop new functional imaging tracers and precursor reagents for the precise diagnosis of lung cancer
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Embodiment 1
[0056] Example 1 Preparation of Compound 1
[0057]
[0058] (1) Synthesis of 5-iodine-7-n-butyl-7H-pirarrol and [2,3-D] pyrimidine 4-chlorine (Compound 4):
[0059] 4-chloro-5-iodo-7H-pyrrole [2,3-D] pyrimidine (Compound 3) (5 g, 17.90 mmol) is mixed with carbonate (11.66 g, 4.66 mmol) mixed in 30 ml DMF and placed in ice water The mixture was cooled to 0 ° C, and iodine n-butane (6.17 mL, 53.7 mmol) was added. After 10 min, the mixture was taken out from ice water to the room temperature seal stirring for 5 h, and the reaction process was detected with TLC. After the reaction is completed, the mixture is cooled and 60 ml of ice water is added, and a precipitate occurs. Abovement, yellow solid (Compound 4) was dried (Compound 4) 5.52 g (yield was 91.9%).
[0070] Tetrate bis (toluenehydrochloride) (164 mg, 3.46 mmol), compound 1 (100 mg, 3.46 mmol) and anhydrouspotassiumcarbonate (100 mg, 3.46 mol) were heated in a 50 mL benzene solution to heat 4 h, 1N HCl Afterward, the reaction mixture was extracted with dichloromethane. The solution was then dried under reduced pressure to give a solid after solidcolumn chromatography (Compound 2) 160 mg (yield of 76%).
[0073] Radionic nuclei marking of Compound 1 figure 1 Ind...
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Abstract
The invention discloses a 7-deaza adenine base as the mother nucleus 18 F‑PET / CT tracer and method for its preparation. The present invention first discloses a compound represented by formula I or a pharmaceutically acceptable salt thereof, wherein, R 1 , R 2 independently selected from H or C 1 -C 5 Alkyl; X is independently selected from 11 C. 18 F. 15 O, or 13 N. The invention also discloses the preparation method and application of the compound represented by formula I. The present invention has successfully prepared a 7-deaza adenine base as the mother nucleus 18 F‑PET / CT Tracers: 18 F‑HX tracer. Experimental result shows, the present invention prepares 18 The uptake of F‑HX tracer in tumor was stable, 3 times higher than in muscle tissue. Therefore, the present invention 18 F‑PET / CT tracers are expected to be applied in PET / CT imaging, changing the situation of lack of tracers in lungcancer.
Description
Technical field [0001] The present invention belongs to the organic chemistry field, and has a parent-based nucleus involving a 7-denitrose adenine base. 18 F-PET / CT tracer and its preparation method thereof. Background technique [0002] PET / CT as a functional imaging advanced diagnosis and treatment equipment, although it is increasingly promoted in lungcancer, it still has great limitations. This limitation is primarily derived from the core components of the functional image: PET / CT tracer. The PET / CT tracer in the current lungcancer is mainly 18 F-FDG, due to 18 F-FDG lacks specificity of other molecular levels other than sugarmetabolism, on the one hand, there is false positive and false negative defects, and on the other hand, it is not possible to reflect the information of the molecular classification or other specific molecular target of lung cancer in the functional imaging level. Major technology bottleneck for precision diagnosis and treatment of lung canc...
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