医药，胰岛素增敏剂，用于治疗糖尿病。
医药
合成路线 1（1. 合成：155141-29-0）
产率：96%
合成条件：for 1 h; Heating; Reflux
实验步骤：实施例3马来酸罗格列酮的制备将93.3g（261.0mmol）实施例2中制备的罗格列酮碱和36.4g（313.2mmol）马来酸悬浮于510mL异丙醇中。将悬浮液加热至回流温度1小时。初始悬浮液变成澄清的无色溶液。将所得溶液冷却至10℃并使用Buechner漏斗过滤。将滤饼用200mL异丙醇洗涤。获得105.0g粗制罗格列酮马来酸盐（85％收率，HPLC纯度为99.57％）。将41.1g（86.9mmol）粗固体和1.7g（14.5mmol）马来酸悬浮于200mL乙醇（每2.3升乙醇0.17当量马来酸，约为马来酸：乙醇比约为13.5） ）。将悬浮液加热至回流温度20分钟。将所得溶液冷却至65℃。将所需的罗格列酮马来酸盐多晶型物的晶种颗粒加入溶液中。将所得悬浮液冷却至0℃并使用Buechner漏斗过滤。将滤饼用50mL乙醇洗涤。得到39.5g马来酸罗格列酮（产率96％，HPLC纯度99.89％），m.p。 120.6-121.7°C
参考文献：
- [1] Patent: US2009/234128, 2009, A1. Location in patent: Page/Page column 5-6 [2] Patent: WO2005/21541, 2005, A2. Location in patent: Page/Page column 15 [3] Patent: EP1468997, 2004, A2. Location in patent: Page 7 [4] Patent: WO2006/125402, 2006, A1. Location in patent: Page/Page column 20 [5] Patent: EP1468997, 2004, A2. Location in patent: Page 7 [6] Patent: EP1468997, 2004, A2. Location in patent: Page 6-7 [7] Patent: EP1468997, 2004, A2. Location in patent: Page 6 [8] Patent: WO2004/62667, 2004, A1. Location in patent: Page/Page column 17 [9] Patent: WO2005/49610, 2005, A1. Location in patent: Page/Page column 15 [10] Patent: WO2006/10653, 2006, A1. Location in patent: Page/Page column 4-5 [11] Patent: EP1468997, 2004, A2. Location in patent: Page 7 [12] Patent: WO2005/21541, 2005, A2. Location in patent: Page/Page column 15 [13] Patent: WO2005/21541, 2005, A2. Location in patent: Page/Page column 15-16 [14] Patent: WO2004/85435, 2004, A1. Location in patent: Page 11 [15] Patent: WO2004/85435, 2004, A1. Location in patent: Page 12-13 [16] Patent: WO2004/85435, 2004, A1. Location in patent: Page 13 [17] Patent: WO2004/85435, 2004, A1. Location in patent: Page 10 [18] Patent: WO2004/85435, 2004, A1. Location in patent: Page 13 [19] Patent: WO2004/85435, 2004, A1. Location in patent: Page 14-15 [20] Patent: WO2004/85435, 2004, A1. Location in patent: Page 11 [21] Patent: WO2004/85435, 2004, A1. Location in patent: Page 10 [22] Patent: WO2004/85435, 2004, A1. Location in patent: Page 13 [23] Patent: WO2005/21541, 2005, A2. Location in patent: Page/Page column 14 [24] Patent: WO2005/21541, 2005, A2. Location in patent: Page/Page column 16 [25] Patent: WO2005/95390, 2005, A2. Location in patent: Page/Page column 16 [26] Patent: WO2005/95390, 2005, A2. Location in patent: Page/Page column 15 [27] Patent: US2007/293546, 2007, A1. Location in patent: Page/Page column 9 [28] Patent: WO2005/49532, 2005, A2. Location in patent: Page/Page column 13-14
