Pafolacianine 化学特性,用途語,生産方法
使用
Pafolacianine is an imaging
agent that has been approved by the FDA for use in fluorescence-guided surgical detection of ovarian cancer. Fluorescence imaging with pafolacianine has the advantages of 1cm deep tissue penetration, low autofluorescence of normal tissue under near-infrared light excitation, long tumour residence time and fast plasma clearance.
合成
The synthesis of pafolacianine started with N10-trifluoroacetylpteroic acid 26.1. This intermediate was obtained by trifluoroacetylation of pteroic acid. Next, product 26.3 was generated in 97% yield by amide coupling reaction with tert-butyl protected tyrosine 26.2. Subsequently, the tert-butyl protecting group was removed using a mixture of trifluoroacetic acid, triisopropylsilane and water (ratio 95:2.5:2.5) to afford compound 26.4. After the trifluoroacetamide group was removed by aqueous sodium hydroxide solution, the attached tyrosine phenoxy group was treated with dye 26.5 to complete the synthesis of 26.
Pafolacianine 上流と下流の製品情報
原材料
準備製品