Preparation method of plerixafor key intermediate

• Main Authors: ZHANG NAIHUA, BAO GUANGLONG
• Format: Patent
• Language: Chinese; English
• Published: 24.11.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of a plerixafor key intermediate. According to the preparation method of the plerixafor intermediate 1, 4, 8, 11-tetraazacyclotetradecane, provided by the invention, N, N '-di (2-ethoxyl)-1, 3-propane diamine is taken as a starting material, hydroxyl is activated by sulfuric acid, then cyclized under an alkaline condition, and then subjected to ring opening and ring expanding cyclization by 1, 3-propane diamine, so that the 1, 4, 8, 11-tetraazacyclotetradecane is prepared. According to the process, introduction and removal of Ts-and other protecting groups are effectively avoided by changing reaction conditions, the operation is simple and convenient, the reaction steps are shortened, the production time is reduced, and the whole synthesis method is simple and convenient to operate and suitable for industrial production. 本发明属于药物合成技术领域，具体涉及一种普乐沙福关键中间体的制备方法。本发明提供的普乐沙福中间体1,4,8,11-四氮杂环十四烷的制备方法，以N,N