The invention discloses beta-(2,3-dihydro-naphthyl[1,2,e]-m-oxazinyl)
tetraphenylporphyrin of which the structural general formula is disclosed as Formula (I) or Formula (II), and a preparation method and application thereof. The preparation method comprises the following steps: 1) preparing 5,10,15,20-tetraphenyl
porphyrin from
pyrrole and
benzaldehyde, carrying out coordination with
copper to obtain 5,10,15,20-tetraphenyl
copper porphyrins, carrying out regioselective
nitration to obtain beta-nitro-substituted-5,10,15,20-tetraphenyl
copper porphyrins, carrying out decoppering and reduction to obtain beta-amino-substituted-5,10,15,20-tetraphenyl porphyrins, and reacting with acetate to obtain beta-amino-substituted-tetraphenyl metalloporphyrins (beta-NH2-MTPP); 2) carrying out
condensation reaction on the beta-NH2-MTPP,
formaldehyde and 2-naphthol, separating the product by
column chromatography to obtain a beta-(2,3-dihydro-1H-naphthyl[1,2,e]-m-oxazinyl)-substituted tetraphenyl
porphyrin metal complex; and decoppering to obtain the beta-(2,3-dihydro-naphthyl[1,2,e]-m-oxazinyl)
tetraphenylporphyrin. The compounds can be used for preparing photodynamic-therapy photosensitizers and
antineoplastic drugs with small toxic and side effects and
high activity.