Design And Synthesis Of Tetrapyrrole Derivatives As Photodynamic New Drugs

Photodynamic therapy(PDT) is a non-invaoive or minimally invasive,non-thermogenesis treatment by destroying the target tissues and cells with photochem reaction.It has many advantages such as good treatment efficiency,mino side effect,simple conditions for treatment compared with traditional treatment.Choosing a suitable photosensitizer is crucial for PDT, which will directly affect the effect of PDT.Most of photosensitizers contain tetrapyrrole structure.There are four drugs containing tetrapyrrole structure in the marketed five photodynamic drugs.At present,the main research is focused on tetraphenylporphyrin,chlorin,alkyl porphyrin and other compounds conjugating with small molecules including steroids,lipids,peptides,nucleosides,nucleotides and the sugar.This paper studied the synthesis of alkyl porphyrin derivatives,tetraphenylporphyrin derivatives and chlorine.A perfect photosensitizer should possess a suitable absorption wavelength which is important to the clinical application.Longer wavelength light absorbed by chlorin photosensitizer due to the reduction of the double bond in pyrrole ring.One hand,photosensitizer must be water-solubility becasue its transfer to the focus is through the blood.On the other hand, photosensitizer must penetrate through the cell wall and has a high selectivity absorption in the cancer cells,so it must be fat-solubility.In this dissertation,the main works are the synthesis of alkyl porphyrin derivatives containing different substitutions and another parts are about modification in tetraphenylporphyrin.In this dissertation,nine new compounds were synthesised including six of alkyl porphyrin derivatives,three of tetraphenylporphyrin derivatives and one chlorine in one year.They were well characterized by 1H NMR and MS.And the studies about PDT for cancers、atrophic arthritis and photodynamic insecticide are in research.