左旋盐酸西替利嗪的制备研究进展-东南大学学报医学版

左旋盐酸西替利嗪的制备研究进展

单位：东南大学化学与化工学院制药工程系

分类号：

出版年·卷·期（页码）：2009·28·第四期（352-357）

摘要：

左旋盐酸西替利嗪(le-vocetirizined ihydrochloride,见图1),化学名为2[-(R)4-[(4-氯苯基)苯甲基]-1-哌嗪基]乙氧基乙酸二盐酸盐,由比利时UCB公司开发,2001年2月首次在德国上市,商品名Xyzal[1]。左旋盐酸西替利嗪属新一代高效无镇静副作用的H1受体拮抗剂,为现临床广泛使用的第二代抗组胺药西替利嗪的R型单一光学异构体,用于治疗过敏性鼻炎和慢性自发性荨麻疹等过敏性疾病[2]。与西替利嗪及其他抗组胺药相比,左旋盐酸西替利嗪具有抗组胺活性强、无镇静副作用、安全性好、临床疗效好、适用人群广泛等优点。目前世界抗过敏药市场主要份额由UCB的西替利嗪和Schering-Plough的氯雷他定占据。西替利嗪是欧洲主要抗组胺药,在我国亦占有压倒性优势。因此开发比西替利嗪作用更强、安全性更好的左旋盐酸西替利嗪,无论从市场前景方面,还是从提高患者临床用药的安全性及有效性方面,均具有深远的意义。1不对称合成Corey等[3]以苯三羰基铬为原料,利用含硼催化剂不对称合成制得左旋盐酸西替利嗪(图2)。苯三羰基铬与等量的叔丁基锂和四甲基乙二胺混合溶液中依次加入CuBr-Me2S和重蒸过的...

参考文献：

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