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    프롤린 화합물의 제조방법
    2.
    发明授权
    프롤린 화합물의 제조방법 无效
    制备脯氨酸化合物的方法

    公开(公告)号：KR1019900002050B1

    公开(公告)日：1990-03-31

    申请号：KR1019870006734

    申请日：1987-06-30

    Applicant: 한국과학기술연구원

    Inventor： 박호군 ,  조정혁 ,  권기탁 ,  강용구

    IPC: C07D207/04

    Abstract: The method for preparing proline compounds of formula (I), used as the inhibitor against angiotensin and antihypertensive agent, is presented. Thus, 4.1g of N-(2-bromopropionyl)-proline benzylester is dissolved in 200 ml of chloroform and the above mixture is cooled in water-ice bath. Then, 1.7g of 2-bromopropionyl chloride is dropped slowly to the 15ml of chloroform solution containing the proline ester. The above mixture is stirred at 25≦̸C for 24 hrs and the obtained chloroform layer is washed with water three times, evaporated and purified using chromatograhy. In (I), R1 and R7 are each H, C1-10 lower alkyl or aryl; R2, R3, R5 and R6 are each H, C1-10 lower alkyl, aryl, amine or cyano ; R4 is H or C1-10 lower alkyl.

    Abstract translation: 提出了制备用于抑制血管紧张素和抗高血压药的式（I）脯氨酸化合物的制备方法。 因此，将4.1g N-（2-溴丙酰基） - 脯氨酸苄基酯溶于200ml氯仿中，将上述混合物在水 - 冰浴中冷却。 然后，将1.7g 2-溴丙酰氯缓慢滴加到15ml含脯氨酸酯的氯仿溶液中。 将上述混合物在25℃下搅拌24小时，所得氯仿层用水洗涤三次，蒸发并用色谱纯化。 在（I）中，R 1和R 7各自为H，C 1-10为低级烷基或芳基; R2，R3，R5和R6各自为H，C1-10低级烷基，芳基，胺或氰基; R4是H或C1-10低级烷基。

    N-(2-할로프로피오닐)-프롤린
    6.
    发明授权
    N-(2-할로프로피오닐)-프롤린 失效
    N-（2-羟基丙酸）丙酯

    公开(公告)号：KR1019900002051B1

    公开(公告)日：1990-03-31

    申请号：KR1019870006973

    申请日：1987-07-01

    Applicant: 한국과학기술연구원

    Inventor： 박호군 ,  조정혁 ,  권기탁 ,  강용구

    IPC: C07D209/04

    Abstract: The method for preparing N-(2-halopropionyl)-proline derivatives of formula (I), used as an inhibitor against angiotensin and antihypertensive agent, is presented. Thus, 4.1g of proline benzylester is dissolved in 20ml of chloroform and the above mixture is cooled in water-ice bath. Then, 1.7g 2-bromopropionyl chloride is dropped slowly in 15ml of chloroform containing proline ester. The above mixture is stirred at 25≦̸C C for 2 hrs and the obtained chloroform layer is washed with water three times, evaporated and purified. In (I), R1 is H, C1-10 lower alkyl or aryl; R2 and R3 are each H, C1-4 alkyl, aryl, amino or cyano; X is Cl, Br or I.

    Abstract translation: 提出了制备用于抑制血管紧张素和抗高血压药的式（I）的N-（2-卤代丙酰基） - 脯氨酸衍生物的方法。 因此，将4.1g脯氨酸苄基酯溶于20ml氯仿中，将上述混合物在水 - 冰浴中冷却。 然后，将1.7g 2-溴丙酰氯缓慢滴入含有脯氨酸酯的15ml氯仿中。 将上述混合物在25℃，C℃下搅拌2小时，所得氯仿层用水洗涤三次，蒸发并纯化。 在（I）中，R 1为H，C 1-10低级烷基或芳基; R2和R3各自为H，C1-4烷基，芳基，氨基或氰基; X是Cl，Br或I.

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