Synthesis Of Small Organic Molecule Probes Focus On The Neurodegenerative Diseases

With the increasing number of aging population, the world-wide aging time is coming. It brings a series of neurodegenerative diseases. One way to diagnosis of these diseases is to know the biological quantitative expression of P-Glycoprotein by PET. Therefore, the main challenge is to find the right tracers. Loperamide, one compound with great research potential, interests many chemists.As a basic skeleton of natural product, quinazoline compounds have a great application in medicine and industry because of great biological activity and pharmaceutical value. In addition, using the waste plant ash in our daily life for chemistry reaction must be a bold attempt.Based on the two directions, we carried out the following researchs.First, we designed and chose an scientific route and prepared a series of loperamide compounds using benzyl cyanide and halogenated pyridine as substrates successfully. Here, we report an effective way for preparing the compounds. Some of them have been used as small molecule probe and showed that they have characteristic function on P-Glycoprotein. It can be used to explore the quantitative analysis of P-Glycoprotein.Second, we have developed a new catalytic system for accomplishing Suzuki coupling reaction of quinazoline-4-tosylates with arylboronic acids in water by utilizing PdCl₂/PPh₃/plant ash?PA? as catalyst. And, we have furnished an access to2,4-diaryl substituted quinazoline derivatives. The reaction system contains several advantages like green, safe, mild reaction conditions, simply operation and good functional group tolerance.