[EN] METHODS OF CHEMICAL SYNTHESIS OF SUBSTITUTED 10H-PHENOTHIAZINE-3,7-DIAMINE COMPOUNDS<br/>[FR] PROCÉDÉS DE SYNTHÈSE CHIMIQUE DE COMPOSÉS SUBSTITUÉS DE 10H-PHÉNOTHIAZINE-3,7-DIAMINE
申请人:WISTA LAB LTD
公开号:WO2017013174A1
公开(公告)日:2017-01-26
The present invention pertains generally to the field of chemical synthesis, and more particularly to methods of chemical synthesis which include the step of preparing a substituted 10H-phenothiazine-3,7-diamine compound of Formula (1) by a step of selective alkylation by reductive amination, in which the corresponding unsubstituted diamine of Formula (4) is reacted with aldehyde/ketone, under reductive amination conditions. The present invention also relates to such methods which incorporate additional subsequent and/or preceding steps, for example, to prepare compounds of Formulae (2) and (3) from compounds of Formula (1), and to prepare compounds of Formula (4) from, for example, compounds of Formulae (5), (6), (7), (8), and (9). Compounds of Formula (1), Formula (2), and Formula (3) are useful, for example, in the treatment of diseases of protein aggregation, such as Alzheimer's disease.
本发明通常涉及化学合成领域,更具体地涉及包括通过还原胺基烷基化步骤来制备配位替代的10H-苯并噻嗪-3,7-二胺化合物的化学合成方法,其中将配位未替代的Formula(4)的二胺与醛/酮在还原胺基化条件下反应。本发明还涉及这种方法,其中包括额外的后续和/或先前步骤,例如,从Formula(1)的化合物制备Formulae(2)和(3)的化合物,以及从Formulae(5)、(6)、(7)、(8)和(9)的化合物制备Formula(4)的化合物。例如,Formula(1)、Formula(2)和Formula(3)的化合物在蛋白质聚集性疾病的治疗中是有用的,例如阿尔茨海默病。