公开(公告)号：US20060111565A1

公开(公告)日：2006-05-25

申请号：US11066511

申请日：2005-02-25

申请人： Ravindra Pandey ,  Andrei Kozyrev ,  Xiang Zheng

发明人： Ravindra Pandey ,  Andrei Kozyrev ,  Xiang Zheng

IPC分类号： C07D487/22

CPC分类号： C07D487/22

摘要： A compound having the structural formula: where R is H or lower alkyl of 1 through 12 carbon atoms. In general, the compounds of the invention are 132-Oxo-bacteriopyropheophorbide-a carboxylic acid and C1-C12 alkyl esters thereof. A method for the preparation of the carboxylic acid compounds of the invention includes the step of reacting bacteriopyropheophorbide-a alkyl ester with lithium hydroxide in tetrahydrofuran and water. A method of the invention for the preparation of the C1-C12 alkyl ester compounds of the invention includes the steps of reacting bacteriopyropheophorbide-a alkyl, especially methyl, ester with lithium hydroxide in tetrahydrofuran and water to obtain 132-Oxo-bacterio-pyropheophobide-a carboxylic acid followed by reacting the carboxylic acid with an acid chloride producing reagent to obtain the 132-Oxo-bacterio pyropheophobide-a acid chloride (compound 5) and reacting the 132-Oxo-bacterio pyropheophobide-a acid chloride with a C1-C12 alcohol to obtain a 132-Oxo-bacterio-pyropheophobide-a carboxylic acid C1-C12 alkyl ester (compound 6). The compounds of the invention may be used as long wavelength absorbing photosensitizers for photodynamic therapy.

摘要翻译： 具有以下结构式的化合物：其中R是H或1至12个碳原子的低级烷基。 一般而言，本发明的化合物是其中一个羧酸和一个C 1 -C 12烷基酯的十二烷基氧杂菌素。 制备本发明的羧酸化合物的方法包括使烷基酯与氢氧化锂在四氢呋喃和水中反应的步骤。 本发明的制备本发明的C 12 -C 12烷基酯化合物的方法包括以下步骤：使抑制甜菜碱 - 烷基，特别是甲基酯与 氢氧化锂在四氢呋喃和水中的溶液，得到13β-氧代 - 焦磷酸酯 - 羧酸，随后将羧酸与产生酰基氯的试剂反应，得到13重量％ > - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - > 12醇，得到13β-氧代 - 焦磷酸酯 - 羧酸C 1 -C 12烷基酯 （化合物6）。 本发明的化合物可用作光动力疗法的长波吸收光敏剂。

公开(公告)号：US07147840B2

公开(公告)日：2006-12-12

申请号：US11066511

申请日：2005-02-25

申请人： Ravindra K. Pandey ,  Andrei Kozyrev ,  Xiang Zheng

发明人： Ravindra K. Pandey ,  Andrei Kozyrev ,  Xiang Zheng

IPC分类号： A61B5/055

CPC分类号： C07D487/22

摘要： A compound having the structural formula: where R is H or lower alkyl of 1 through 12 carbon atoms. In general, the compounds of the invention are 132-Oxo-bacteriopyropheophorbide—a carboxylic acid and C1–C12 alkyl esters thereof. A method for the preparation of the carboxylic acid compounds of the invention includes the step of reacting bacteriopyropheophorbide—a alkyl ester with lithium hydroxide tetrahydrofuran and water. A method of the invention for the preparation of the C1–C12 alkyl ester compounds of the invention includes the steps of reacting bacteriopyropheophorbide—a alkyl, especially methyl, ester with lithium hydroxide in tetrahydrofuran and water to obtain 132-Oxo-bacterio-pyropheophobide-a carboxylic acid followed by reacting the carboxylic acid with an acid chloride producing reagent to obtain the 132-Oxo-bacterio pyropheophobide-a acid chloride (compound 5) and reacting the 132-Oxo-bacterio pyropheophobide-a acid chloride with a C1–C12 alcohol to obtain a 132-Oxo-bacterio-pyropheophobide-a carboxylic acid C1–C12 alkyl ester (compound 6). The compounds of the invention may be used as long wavelength absorbing photosensitizers for photodynamic therapy.

摘要翻译： 具有以下结构式的化合物：其中R是H或1至12个碳原子的低级烷基。 一般而言，本发明的化合物是其中一个羧酸和一个C 1 -C 12烷基酯的十二烷基氧杂菌素。 制备本发明的羧酸化合物的方法包括使烷基酯与氢氧化锂四氢呋喃和水反应的步骤。 本发明的制备本发明的C 12 -C 12烷基酯化合物的方法包括以下步骤：使抑制甜菜碱 - 烷基，特别是甲基酯与 氢氧化锂在四氢呋喃和水中的溶液，得到13β-氧代 - 焦磷酸酯 - 羧酸，随后将羧酸与产生酰基氯的试剂反应，得到13重量％ > - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - > 12醇，得到13β-氧代 - 焦磷酸酯 - 羧酸C 1 -C 12烷基酯 （化合物6）。 本发明的化合物可用作光动力疗法的长波吸收光敏剂。