AIM: To search for new photosensitizers for photodynamic therapy (PDT) of cancer. METHODS: Chlorin f methyl ether (1) is synthesized via addition and nucleophilic substitution reaction of 2 vinyl of chlorin f (3) whic...AIM: To search for new photosensitizers for photodynamic therapy (PDT) of cancer. METHODS: Chlorin f methyl ether (1) is synthesized via addition and nucleophilic substitution reaction of 2 vinyl of chlorin f (3) which was prepared through acidic and alkaline oxidative degradation using silkworm excrement crude chlorophyll extracts as starting material. RESULTS: Compounds 1 and 2 are new compounds. Preliminary sensitizing effects on photooxidation of NADPH in D 2O and photodynamic effects for transplanted sarcoma S 180 in mice of compound 1 were shown to be stronger than those of hematoporphyrin derivative (HpD) and compound 3. CONCLUSION: It is suggested that compound 1 is possible to be developed as a new photosensitizer for PDT of cancer.展开更多
A novel synthesis process of 5H-dibenz[b,f]azepine was studied.It is an important intermediate of 5H-dibenz[b,f]azepine-5-carboxamide,used in genetic engineering,materials science and so on.With 10,11-dihydro-5H-diben...A novel synthesis process of 5H-dibenz[b,f]azepine was studied.It is an important intermediate of 5H-dibenz[b,f]azepine-5-carboxamide,used in genetic engineering,materials science and so on.With 10,11-dihydro-5H-dibenz[b,f]azepine as raw material,5-chloroformyl-5H-dibenz[b,f]azepine was prepared by reflux with triphosgene in toluene,brominated with bromine in chlorobenzene,and dehydrobrominated at 130℃,finally,the title compound was obtained by removing chloroformyl group with NaOH in isopropanol with 80.4% overall yield.The optimal reaction conditions and yields (temperature,time,molar yield) were as follows: acyl chlorination,110℃,10 h,93.0%; bromination,dehydrobromination,100℃,2 h,130℃,5 h,88.0%; removal of chloroformyl group,40℃,3 h,98.2%. The melting point of the title compound was the same as literature reported,and its structure was confirmed by 1H NMR.The optimal technology condition to remove chloroformyl group as protection group and its application of protection for some amine compounds were also studied.展开更多
文摘AIM: To search for new photosensitizers for photodynamic therapy (PDT) of cancer. METHODS: Chlorin f methyl ether (1) is synthesized via addition and nucleophilic substitution reaction of 2 vinyl of chlorin f (3) which was prepared through acidic and alkaline oxidative degradation using silkworm excrement crude chlorophyll extracts as starting material. RESULTS: Compounds 1 and 2 are new compounds. Preliminary sensitizing effects on photooxidation of NADPH in D 2O and photodynamic effects for transplanted sarcoma S 180 in mice of compound 1 were shown to be stronger than those of hematoporphyrin derivative (HpD) and compound 3. CONCLUSION: It is suggested that compound 1 is possible to be developed as a new photosensitizer for PDT of cancer.
文摘A novel synthesis process of 5H-dibenz[b,f]azepine was studied.It is an important intermediate of 5H-dibenz[b,f]azepine-5-carboxamide,used in genetic engineering,materials science and so on.With 10,11-dihydro-5H-dibenz[b,f]azepine as raw material,5-chloroformyl-5H-dibenz[b,f]azepine was prepared by reflux with triphosgene in toluene,brominated with bromine in chlorobenzene,and dehydrobrominated at 130℃,finally,the title compound was obtained by removing chloroformyl group with NaOH in isopropanol with 80.4% overall yield.The optimal reaction conditions and yields (temperature,time,molar yield) were as follows: acyl chlorination,110℃,10 h,93.0%; bromination,dehydrobromination,100℃,2 h,130℃,5 h,88.0%; removal of chloroformyl group,40℃,3 h,98.2%. The melting point of the title compound was the same as literature reported,and its structure was confirmed by 1H NMR.The optimal technology condition to remove chloroformyl group as protection group and its application of protection for some amine compounds were also studied.
