论文部分内容阅读
本文从十六种保护氨基的方法中选择了以茴香醛与氨基缩合形成西佛碱的办法来保护氨基。此法在氢氧化钠水溶液中引入保护基并用盐酸以解除保护基。这两步反应收率较高,简便易行,与Baba等所介绍的方法相比,总收率高4%以上。中间体2—0—苯甲基—4—0—(2—脱氧—2—对—甲氧苯甲叉基—3,4,6—三—0—乙酰基—β—D—葡糖基)—5—氟脲嘧啶(Ⅴ)是末见报道过的新化合物。(Ⅴ)和解除保护基团后得到的产物2—0—苯甲基—4—0—(2—脱氧—2—氨基—3,4,6—三—0—乙酰基—β—D—葡糖基)—5—一氟脲嘧啶盐酸盐(Ⅵ),其分子量和结构,均经元素分析、质谱、红外光谱和核磁共振谱等加以证实。同时,还确定了(Ⅴ)的构型属β—型。
This article from sixteen kinds of methods to protect the amino group was chosen anisaldehyde and amino condensation to form sifu alkali way to protect the amino. This procedure introduces a protecting group in aqueous sodium hydroxide and hydrochloric acid to unblock the protecting group. The two-step reaction yield is high, simple and easy, compared with Baba and other methods introduced, the total yield higher than 4%. Intermediate 2-0-Benzyl-4-O- (2-deoxy-2-p-methoxybenzylidene-3,4,6-tri-O-acetyl-β-D-glucosyl ) -5-Fluorouracil (V) is a novel compound reported previously. (V) and the product 2-0-benzyl-4-O- (2-deoxy-2-amino-3,4,6-tri-O-acetyl-β-D- Glucosyl) -5-fluorouracil hydrochloride (Ⅵ), its molecular weight and structure were confirmed by elemental analysis, mass spectrometry, infrared spectroscopy and nuclear magnetic resonance spectroscopy. At the same time, it has also been confirmed that the configuration of (V) is a β-type.