2908-71-6Relevant academic research and scientific papers
RADIOISOTOPE 18F SUBSTITUTED THIAMINE, AND SYNTHESIS METHOD AND USE THEREOF
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, (2018/09/12)
The present invention discloses a radioisotope 18F substituted thiamine, synthesis method, and use thereof in small animal PET/CT imaging. The radioisotope 18F substituted thiamine has a structure of The synthesis method comprises radiochemical synthesis by using existing precursors. In the present invention, the hydroxyl in the hydroxyethyl on the thiazole cycle of thiamine is replaced by radioisotope 18F, to prepare a PET tracer. The radioisotope 18F substituted thiamine of the present invention successfully enters the brains of various strains of mice, and the uptake in the brains of thiamine-deficient mice is obviously greater than that in normal control. The present invention is useful in the preparation of a brain imaging tracer for clinical trials of Alzheimer's disease and tumors.
Synthesizing method for 4-amino-2-methyl-5-(brooethyl) pyrimidine hydrobromide
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Paragraph 0031; 0032-0086; 0091; 0096; 0101, (2018/03/01)
The invention discloses a synthesizing method for 4-amino-2-methyl-5-(brooethyl) pyrimidine hydrobromide. The method comprises the following steps: acquiring formylated midbody sodium salt A by reacting 3-methoxypropionitrile with ethyl formate under the effect of sodium methylate; reacting the midbody sodium salt A with dimethyl sulfate, thereby acquiring a midbody B; condensing the midbody B with acetamidine hydrochloride, thereby acquiring a midbody C; and reacting the midbody C with hydrobromic acid, thereby acquiring a target product 4-amino-2-methyl-5-(brooethyl) pyrimidine hydrobromide I. According to the invention, the raw material source is wide and the cost is low; the synthesizing method is simple in production operation and has low requirement for processing equipment; the rigorous production conditions, such as, anhydrous condition, anaerobic condition and high-pressure hydrogenation, are not required; the reaction condition is mild; the method is easy for large-scale industrial production; the process is simple; the production period is short; the production efficiency is high; the production method is green and environmentally friendly and is suitable for large-scale industrial production.
