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    • 5. 发明公开
    • (+)-시스-서트랄린의 선택적인 제조방법
    • (+) - CIS-丝氨酸的选择性制备方法
    • KR1020130051758A
    • 2013-05-21
    • KR1020110117089
    • 2011-11-10
    • 보령제약 주식회사
    • 김제학이준광선용호이성국남은혜
    • C07C209/88C07C211/42A61K31/13A61P25/24
    • PURPOSE: A manufacturing method of a (+)-cis-sertaline is provided to manufacture (+)-cis-sertaline of high purity and high yield which does not includes dechlorinated sertaline byproduct, by selectively separating and purifying only a (+)-cis-sertaline. CONSTITUTION: A manufacturing method of a (±)-cis-sertaline represented by chemical formula 1 comprises: a step of manufacturing (+)-cis-sertaline (S)-(-)-2-pyrrolidone-5-carboxylate by reaction of (±)-cis/trans-sertaline represented by chemical formula 2 or (±)-cis-sertaline and (S)-(-)-2-pyrrolidone-5-carboxylate and optically dividing the product. The use amount of the (S)-(-)-2-pyrrolidone-5-carboxylate is 0.25-1.0 molar equivalent, based on 0.25-1.0 molar equivalent. The reaction solvent is selected from toluene, ethylacetate, acetone, and ethanol.
    • 目的:提供(+) - 顺式 - 西他列胺的制备方法,通过选择性分离和纯化(+) - 顺式 - 胺甘氨酸来制备高纯度和高产率的(+) - 顺式胺,不含脱氯的sertaline副产物, 顺式舍曲林。 构成:由化学式1表示的(±) - 顺式 - 丝氨酸的制造方法包括:通过以下步骤制备(+) - 顺式 - 西他宁(S) - ( - ) - 2-吡咯烷酮-5-羧酸酯的步骤: 以(±) - 顺式胺和(S) - ( - ) - 2-吡咯烷酮-5-羧酸酯为代表的(±) - 顺/反 - (S) - ( - ) - 2-吡咯烷酮-5-羧酸酯的使用量为0.25-1.0摩尔当量,基于0.25-1.0摩尔当量。 反应溶剂选自甲苯,乙酸乙酯,丙酮和乙醇。