College of Pharmacy, Seoul National University, 1 Gwanak-ro, Gwanak-gu, Seoul 08826, Korea.
Department of Synthetic Chemistry, Chong Kun Dang Research Institute, 315-20, Dongbaekjukjeon-daero, Giheung-gu, Yongin-si 16995, Gyeonggi-do, Korea.
Molecules. 2017 Nov 15;22(11):1971. doi: 10.3390/molecules22111971.
A practical and sustainable method for the synthesis of levocabastine hydrochloride (), a H₁ receptor antagonist for the treatment of allergic conjunctivitis, that can be applied to the industrial production of the compound has been developed. Substantial improvements over the previously reported procedure are achieved via efficient preparation of an optically active key intermediate () without chiral resolution and with a more effective detosylation, which complements the previous procedure. Notably, our process requires no chromatographic purification and provides levocabastine hydrochloride in greater than 99.5% purity in a 14.2% overall yield.
已开发出一种实用且可持续的方法来合成盐酸左卡巴斯汀（），这是一种用于治疗过敏性结膜炎的 H₁受体拮抗剂，可以应用于该化合物的工业生产。与之前报道的方法相比，通过有效制备光学活性关键中间体（）而无需手性拆分且脱酯化更有效，从而实现了实质性改进，这补充了之前的方法。值得注意的是，我们的工艺不需要进行色谱纯化，并且以 14.2%的总收率提供了超过 99.5%纯度的盐酸左卡巴斯汀。
