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(R)-卡尼丁(维生素BT,康胃素,7)可转化体内贮存的脂肪为能量,因而可治疗心脏病,高血脂病,也可用作运动员以及婴儿的营养品等。过去光学活性卡尼丁的制备通常都是合成混旋体或混旋前体,再进行拆分。本文报道了以(R)-苹果酸为原料,用苯甲醇酯化得(R)-苹果酸二酯,再经BMS/NaBH_4选择性还原成单酯(R)-3。(R)-3,依次经单对甲苯磺酰化、三甲胺取代、钯碳脱苄基以及离子交换得7。六步反应,收率较高,可以大规模生产。(S)-卡尼丁可以类似合成。
(R) - Carnitine (vitamin BT, Kang Wei Su, 7) can be transformed into fat stored in the body as energy, which can treat heart disease, hyperlipidemia, but also can be used as athletes and infants nutrition. In the past, the preparation of optically active carnitine was usually a synthetic or mixed precursor, which was then resolved. In this paper, (R) - malic acid diester was esterified with benzyl alcohol using (R) - malic acid as starting material and then selectively reduced to monoester (R) -3 by BMS / NaBH4. (R) -3, followed by mono-p-tosylate, trimethylamine, palladium on carbon, and ion-exchanged. Six-step reaction, higher yield, can be large-scale production. (S) -caridin can be synthesized in a similar manner.