Method for preparing cariprazine and intermediate thereof

• Main Authors: TIAN, GUANGHUI, ZHANG LIJUN, XING XINGLONG
• Format: Patent
• Language: Chinese; English
• Published: 01.04.2022
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention relates to a method for preparing cariprazine and an intermediate thereof, and the method comprises the following steps: taking trans-4-aminocyclohexane acetate hydrochloride as a starting material, and carrying out Boc protection, reduction, halogenation, nucleophilic substitution, Boc protection removal and amidation reaction to prepare the cariprazine. The alcoholic hydroxyl group of the trans-2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl} ethanol is activated and converted into a group easy to leave, the alcoholic hydroxyl group is creatively converted into the halogen atom, the reaction condition is mild, the yield is high, the raw material medicine which is high in purity and low in impurity content and meets the medicinal requirement can be obtained, and the method is suitable for industrial production. 本发明涉及一种制备卡利拉嗪及其中间体的方法，包括如下步骤：以反式-4-氨基环己烷乙酸酯盐酸盐为起始物料，通过Boc保护、还原、卤代、亲核取代、脱Boc保护和酰胺化反应制备得到卡利拉嗪。本发明将反式2-{1-[4-(N-叔丁氧基羰基)-氨基]-环己基}乙醇的醇羟基活化转化成易于离去的基团，创造性地将醇羟基转换为卤素原子，反应条件温和，收率高，可以得到纯度高、杂质含量低