Focal Methyl Magnesium Chlorophyllinoff-a Single Hydrazone Derivativesand Optical Properties

Photodynamic therapy(photodynamic therapy, called PDT) is a new method for treating tumor diseases.It uses a combination of light,oxygen and selectively aggregated photosensitizer in tumor cells,it can selectively kill tumor cells. Photo dynamic therapy consists of three main factors:light, photosensitizer and oxygen.The photosensitizer is the core material, according to the requirements photodyna mic therapy, in clinical,the ideal photosensitive drugs should have the following c haracteristics:1. in the wavelength range of 600-850 nm has strong absorption an d less tissue scatters light phototherapy in the window, and the competitive subst ance of endogenous small absorption, thus making the illumination light to penet rate the deep tissue, so that the role of photodynamic therapy is effective in the treatment of neoplastic disease. 2.The triplet energy is greater than 94 KJ / mol,high quantum yield. In the PDT process, the photo-excited singlet state, through intersystem crossing into a triplet photosensitizer. 3. The high selectivity. Photos ensitizer can be selectively gathered and distributed in normal tissues with little or no distribution is an important foundation to achieve good efficacy. It can Sel ectively kill the tumor, especially in the skin, the requirements of photosensitizer concentration is low, to reduce the generation of photosensitive dermatitis effect.Methyl Pyropheophorbide-a is a degradation product of chlorophyll,in its absorpti on spectrum,it has a strong absorption peak at 667 nm and in the visible(red) e xcitation, which has a strong fluorescence at 670 nm emission intensity, thus mo difying the outer peripheral ring of Pyropheophorbide-a, expanding large π-conjug ated system,it is possible to obtain a series of new compoundswhich has a large absorption wavelength.Studying the spectral properties of these derivatives, we may get more penetrating new PDT photosensitizers. Therefore, this article from the mehyl Pyropheophorbide-a respectively with o-trifluoromethylphenyl hydrazine,phenylhydrazine trifluoromethyl,p-bromophenyl hydrazine,p-fluorophenyl hydrazine,we respectively get methyl Pyropheophorbide-a o-trifluoromethylphenylhydrazono(6a),methyl Pyropheophorbide-a trifluoromethylphenylhydrazono(6b), methyl Pyropheophorbide-a p-bromo hydrazone(6c),methyl Pyropheophorbide-a fluorobenzohydraz onoyl(6d), focusing methyl pheophorbide-a-131-,the maximum absorption waveleng th of such compounds 6a~6d from 668 nm respectively increased to 683 nm,the photosensitizers enhanced penetration.We test the spectral properties of methyl P yropheophorbide–a single hydrazone derivatives 6a-6d, respectively, in methylene chloride, methanol, ethanol, N,N- dimethylformamide, toluene, n-hexane, and the condition- visible absorption and fluorescence spectra of pH = 2,3,4,5,6,7,8, 9,10. The results showed that methyl Pyropheophorbide –a single hydrazone derivat ives 6a-6d have a strong UV absorption, and with the increase of solvent pH va lues, have emerged red shift.The fluorescence intensity of methyl Pyropheophorbi de–a single hydrazone derivatives 6a-6d is strong,the methyl Pyropheophorbide–a single hydrazone derivatives 6a-6d are good photosensitizer,they can be applied in photodynamic therapy as well as in medical fluorescence imaging.All structures of the new compounds are tested by NMR, MS.