(A) The Preparation of Radiopharmaceutical for the Imaging of Cardiac β-Adrenoceptors (B) An Attempt to Synthesize Compound with 1,2,5-thiadiazole Partial Structure

• Main Authors: Tseng Wen Hsiung, 曾文雄
• Other Authors: Yang Chia Hsi
• Format: Others
• Language: zh-TW
• Published: 1999
• Online Access: http://ndltd.ncl.edu.tw/handle/58958311834446193929

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 .