Methods of chemical synthesis of substituted 10H-phenothiazine-3,7-diamine compounds
申请人:WisTa Laboratories Ltd.
公开号:US10323010B2
公开(公告)日:2019-06-18
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.
本发明一般涉及化学合成领域,更具体地说,涉及化学合成方法,其中包括通过还原胺化选择性烷基化步骤制备取代的式(1)10H-吩噻嗪-3,7-二胺化合物,在还原胺化条件下,相应的式(4)未取代二胺与醛/酮反应。本发明还涉及包含额外后续步骤和/或前述步骤的此类方法,例如,由式(1)化合物制备式(2)和(3)化合物,以及由式(5)、(6)、(7)、(8)和(9)化合物制备式(4)化合物。式(1)、式(2)和式(3)化合物可用于治疗蛋白质聚集性疾病,如阿尔茨海默病。