卡泊三醇的合成研究进展  

Research advance on the synthesis of calcipotriol

作　　者：王文彬[1] 张凡[1] 何祥[1] 林华清[2] 张佳[2] 黄年玉[1] 

机构地区：[1]三峡大学生物与制药学院,湖北宜昌443002 [2]湖北恒安药业有限公司,湖北宜昌443103

出　　处：《化学研究与应用》2016年第6期764-769,共6页Chemical Research and Application

基　　金：国家自然科学基金项目(21102084)资助;三峡大学青年拔尖人才培育基金;研究生科研创新基金项目(2015CX131)资助

摘　　要：银屑病是临床中极为常见的慢性红斑鳞屑性皮肤病,在全球范围内均有较高的发病率。卡泊三醇在1987年由Leo公司首先研发,卡泊三醇软膏剂在1996年获得美国FDA批准上市。作为一类活性维生素D3类似物,卡泊三醇能够诱导角质细胞的分化、抑制其增殖、调节免疫功能并减轻炎症,是治疗银屑病的一线药物。本文综述了近20年来国内外关于卡泊三醇的合成方法,并就其关键中间体C24-OH的手性构建及拆分方法进行了总结,为卡泊三醇的合成工艺开发和工业应用提供了参考。Psoriasis is a common and chronic inflammatory skin disease most often appearing in the form of well-demarcated,scaly plaques.There is a highly incidence for psoriasis all over the world.Calcipotriol was firstly developed by Leo Pharma A/S in 1987,and calcipotriol cream was approved by FDA in 1996. As the hormonally active form of vitamin D,calcitriol had become a first-line treatment for psoriasis,which was well known for its diverse pharmacological activities including promoting the differentiation of keratinocytes,inhibiting the proliferation of these cells,modulating immune function and reduction of inflammation.The purpose of this review was to summarize the recent two decades＇ advance on the synthetic and separating methods for calcitriol and its key intermediates,and provided data for the development and industrial application of the drug.

关 键 词：银屑病 卡泊三醇 合成工艺 手性还原 研究进展 

分 类 号：O622.3[理学—有机化学]