卡利拉嗪关键中间体的合成工艺研究

Study on the Synthesis of Cariprazine Key Intermediates

标题化合物可作为非典型抗精神病药卡利拉嗪的关键中间体。以廉价易得的4-N-Boc-氨基环己酮(2)为起始原料,经过Wittig-Horner、酯键还原、双键还原及手性拆分得到标题化合物。通过单因素实验,研究了前三步反应的关键影响因素,得到了适宜的合成条件,标题化合物的收率31.5%(以4-N-Boc-氨基环己酮计),适合工业化生产。

The title compound serves as a key intermediate for the atypical antipsychotic calidrin. In this paper, 4-N-Boc-aminocyclohexanone(2), which is a cheap and readily available compound, was used as a starting material to give the title compound via Wittig-Horner, ester bond reduction, double bond reduction and chiral resolution. Through the single factor experiment, the key influencing factors of the first three steps were studied, and the suitable synthesis conditions were obtained. The yield of the title compound was 31.5%(based on 4-N-Boc-aminocyclohexanone), which was suitable for industrial production.