Processes for large scale production of tetrapyrroles

Details Processes for large scale production of tetrapyrroles Processes for large scale production of tetrapyrroles

C - Chemistry, Metallurgy

07

D

C07D 487/22 (2006.01) A61K 41/00 (2006.01) C07D 209/00 (2006.01) C07D 257/00 (2006.01)

Patent

CA 2435488

The present invention relates to processes especially suitable for the large scale production of tetraphyrrolic compounds, such as meso-formyl porphyrins, mesoacrylate porphyrins, purpurins and benzochlorins. In particular, tin ethyl etiopurpurin (SnET2), sometimes called rostaporfin, and the intermediates necessary for its production without chromatography are disclosed. In addition, much of the chemistry disclosed is applicable to the large scale manufacturing of benzochlorins. Purpurins, benzochlorins and several of the intermediates in the synthesis may be useful as photosensitizers in photodynamic therapy, or as porphyrin building blocks in the synthesis of other porphyrinic materials.

L'invention a trait à des procédés particulièrement adaptés à la production à grande échelle de composés tétrapyrroliques, tels que les meso-formyl-porphyrines, les meso-acrylate-porphyrines, les purpurines et les benzochlorines. L'invention concerne en particulier la tin-éthyl-étiopurpurine (SnET2), appelée parfois rostaporfine, et les intermédiaires nécessaires à sa production sans chromatographie. En outre, une grande partie des procédés chimiques décrits sont applicables à la fabrication à grande échelle de benzochlorines. Des purpurines, des benzochlorines et plusieurs intermédiaires dans leur synthèse peuvent être utiles en tant que photosensibilisateurs dans la thérapie photodynamique, ou en tant qu'éléments constitutifs de porphyrines dans la synthèse d'autres matériaux porphyriniques.

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