A new manufacturing process for N-[[1-(methylamino)cyclopropyl]methyl]pyridine-3-amine hemigalactarate (1) has been developed. Herein we wish to report the development and optimization of the route using alternative reaction conditions for a reduction/oxidation/reductive amination/protecting group cleavage sequence. Improvement of the crystallization process enabled the production of multikilogram amounts of agonist 1 under cGMP control with a purity of >99.5%. A telescoped process involving 5 steps is also described.

中文翻译：

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有效合成乙酰胆碱烟碱受体激动剂的进展

已开发出N -[[[（（（甲基氨基）环丙基）甲基]吡啶-3-胺半乳酸酯（1）的新制造方法。在此，我们希望报告使用用于还原/氧化/还原胺化/保护基裂解序列的替代反应条件开发和优化路线的方法。结晶过程的改进使得能够在cGMP控制下生产多千克量的激动剂1，其纯度> 99.5％。还描述了涉及5个步骤的伸缩过程。