乐伐替尼甲磺酸盐是一种合成的口服活性酪氨酸激酶抑制剂，可抑制血管内皮生长因子受体(VEGFR1-3)、成纤维细胞生长因子受体(FGFR1-4)、血小板衍生生长因子受体(PDGFRα)、干细胞因子受体(Kit (c-Kit))及转染重排(RET (c-RET))，具有潜在抗肿瘤活性，用于中晚期肝细胞癌等癌症的治疗，临床试验显示其优于标准治疗药物索拉非尼。
医药
合成路线1
- 原料：4-[3-氯-4-(环丙基氨基羰基)氨基苯氧基]-7-甲氧基-6-喹啉甲酰胺（23.0kg）、甲磺酸（5.44kg+777g）、乙酸（150L+11.5L）、1-丙醇（46.0L+161L）、23%乙酸异丙酯（115L）、乙醇（173L）
- 步骤：在20-35℃下，将4-[3-氯-4-(环丙基氨基羰基)氨基苯氧基]-7-甲氧基-6-喹啉甲酰胺溶解于甲磺酸和乙酸混合溶液中；加入甲磺酸后，35℃以下过滤，乙酸洗涤；滤液25-45℃加入1-丙醇和晶种，再加入1-丙醇和23%乙酸异丙酯；冷却至15-25℃，过滤，用1-丙醇和乙酸异丙酯混合溶液（1-丙醇33v/v%）洗涤；湿晶体加乙醇，20-60℃搅拌3小时，过滤，乙醇洗涤，80℃以下减压干燥
- 条件：温度范围20-35℃（溶解）、35℃以下（过滤）、25-45℃（加溶剂）、15-25℃（冷却结晶）、80℃以下（干燥）
- 收率：94%（27.5kg）
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