Summary: | 碩士 === 中原大學 === 化學系 === 88 === ﹙A﹚The purpose of this project is to synthesize CYBL4E, an antagonist of cardiac β-adrenoceptor, which can be used as an imaging agent for heart. To synthesize CYBL4E, 2-amino-3- nitrophenol is used as the starting material. The starting material is first transform to 1-(2-Amino-3-Nitrophenoxyl)-2’,3’- Epoxypropane .The substituent at 1-position is transformed to 3’-(Propargylamino)-2’- Propanol by the reaction of propargyl amine with the previous product. Reduction of the nitro group at 3-position converts the product in previous step into a 2,3-diamino compound. The reaction of phosgene with the 2,3-diamino compound gives 4-(3’-Propargylamino-2’-Hydroxypropoxyl)- Benzimidazol-2-one. The reaction of tributyltin chloride with the triple bond in the propargyl group converts this functional group to a tributylstannyl ethenyl group and give the precursor for imaging agent.
﹙B﹚ Urea , thionyl chloride , pyridine and α-Naphthoquinone in different conditions are allowed to react and Naphtho[2,3-c]- [1,2,5]thiadiazole-4,9-dione was obtained .
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