生命科学；医药，用于治疗前列腺增生症和高血压。
医药
合成路线 1（1. 合成：81403-68-1）
产率：87.5%
合成条件：Stage #1: With sodium hydroxide In dichloromethane; water at 20℃; for 0.50 h; Stage #2: With hydrogenchloride In ethanol; dichloromethane
实验步骤：在搅拌下，向2L四颈烧瓶中分批加入320mL水和142g阿夫唑嗪磺酸盐。将35ml的30％NaOH和1420mL的CH 2 Cl 2加入到所得溶液中，并将两相溶液在约20℃的温度下保持搅拌30分钟。停止搅拌，分离各相，用350mL H 2 O萃取有机相，然后用4g硅沸石和4g脱色碳处理约30分钟。过滤弃去固体残余物，用70mL CH 2 Cl 2洗涤。将合并的有机相装入2L反应器中，并加入100g约8.5％HCl / EtOH溶液。将如此得到的溶液浓缩，直至通过减压蒸馏和保持约20℃的内部温度达到最小可搅拌量。然后加入300毫升EtOH，在大气压下将物料加热至80℃，同时蒸馏除去溶剂。将物料保持在这样的温度直至获得约300mL的残余物。停止蒸馏，将物料在约20℃下冷却1小时，然后过滤，用50mL EtOH洗涤板。将得到的结晶固体在50℃下真空干燥约12小时，得到85g（ 0.199摩尔）[N1-（4-氨基-6,7-二甲氧基喹唑-2-基）-N1-甲基-N2-（四氢 - 呋喃基-2） - 丙二胺]盐酸盐（阿夫唑嗪盐酸盐），为白色结晶固体。盐酸阿夫唑嗪：产率87.5％; HPLC测定纯度为99.8％
参考文献：
- [1] Patent: WO2010/10058, 2010, A1. Location in patent: Page/Page column 13; 14
合成路线 2（2. 合成：81403-68-1）
产率：88%
合成条件：With hydrogenchloride In ethanol at 20 - 25℃;
实验步骤：实施例4：无水阿夫唑嗪盐酸盐的制备：将阿夫唑嗪碱（5g，0.013mol）加入烧瓶中，加入乙醇（110ml）。 将混合物回流15分钟。 并且固体溶解了。 将活性炭加入该溶液中，将悬浮液搅拌10分钟，过滤并用5ml热乙醇洗涤。 将滤液冷却至20-25℃并加入用氯化氢气体（1.5ml）饱和的乙醇。 然后将二乙醚（25ml）和水（0.09ml）缓慢加入混合物中。 然后将混合物在室温下搅拌20小时。 然后将混合物冷却至0-5℃，搅拌1小时后滤出产物，用7.5ml乙醚洗涤。 将结晶产物在真空干燥器中在120℃下干燥最少8小时。 阿夫唑嗪盐酸盐的产量为4.85g（88％）。
参考文献：
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