会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明申请
    • PROCESS FOR THE PREPARATION OF CHIRAL GLYCIDYLPHTHALIMIDE IN HIGHLY OPTICAL PURITY
    • 在高光学纯度下制备丙二酰胆碱酯酶的方法
    • WO2007132990A1
    • 2007-11-22
    • PCT/KR2007/002154
    • 2007-05-02
    • RSTECH CORPORATIONKANG, Hyun BinQUAN, Long GuoLEE, Jae KwanKIM, Seong-Jin
    • KANG, Hyun BinQUAN, Long GuoLEE, Jae KwanKIM, Seong-Jin
    • C07D405/06
    • C07D405/06
    • The present invention relates to a process for the preparation of highly optical pure glycidylphthalimide. More particularly, the present invention relates to a process for the preparation of chiral glycidylphthalimide, which comprises the steps of reacting an optically active 3-susbstituted 1-amino-2-propanol acid addition salt with phthalic anhydride in a presence of a base to obtain N -(3-substituted-2-hydroxypropyl)phthalimide and subjecting the obtained compound to an epoxide cyclization reaction to prepare the targeted glycidylphthalimide. According to the process, the chirality of the starting material is substantially retained throughout overall procedures. Therefore, the process can prepare the targeted glycidylphthalimide in an optically pure form having 99%ee or higher. And, the reactions are carried out under mild conditions through overall procedures and in a single reaction vessel without any special purification. This increases the yield of the target compound.
    • 本发明涉及制备高光学纯缩水甘油基邻苯二甲酰亚胺的方法。 更具体地说,本发明涉及手性缩水甘油基邻苯二甲酰亚胺的制备方法,该方法包括以下步骤:在碱的存在下使光学活性的3-取代的1-氨基-2-丙醇酸加成盐与邻苯二甲酸酐反应,得到 N-(3-取代-2-羟基丙基)邻苯二甲酰亚胺,并使所得化合物进行环氧化物环化反应,制备目标缩水甘油基邻苯二甲酰亚胺。 根据该方法,起始原料的手性基本上保留在整个方法中。 因此,该方法可以制备具有99%ee或更高的光学纯形式的目标缩水甘油基邻苯二甲酰亚胺。 而且,反应在温和条件下通过总体程序和在单个反应容器中进行而没有任何特别的纯化。 这增加了目标化合物的产率。
    • 6. 发明申请
    • PROCESS FOR THE EFFICIENT PREPARATION OF 3-HYDROXY PYRROLIDINE AND DERIVATIVES THEREOF
    • 有效制备3-羟基吡咯烷及其衍生物的方法
    • WO2009011551A3
    • 2009-03-12
    • PCT/KR2008004193
    • 2008-07-17
    • RSTECH CORPQUAN LONG GUOLEE JAE KWANHONG MEI HUAKIM KWANG SUBPARK KWANG SIK
    • QUAN LONG GUOLEE JAE KWANHONG MEI HUAKIM KWANG SUBPARK KWANG SIK
    • C07D207/12
    • C07D207/12
    • The present invention relates to an effective process for the preparation of 3-hydroxypyrrolidine or derivatives thereof. The process comprises (a) protecting a hydroxyl group of 4-halo-3-hydroxybutyric acid, (b) reducing an ester group of the compound obtained from the step (a) to obtain a corresponding alcohol compound, (c) reacting the compound obtained from the step (b) with sulfonyl halide to produce a corresponding sulfonate compound, (d) reacting the compound obtained from the step (c) with an amine to obtain 3-hydroxy-protected pyrrolidine compound, and (e) deprotecting the compound obtained from the step (d) to produce the targeted 3-hydroxypyrrolidine or derivatives thereof. The process provides 3-hydroxypyrrolidine or derivatives thereof with high optical purity, because optical purity of the starting material is substantially retained. In the process, each of the steps is carried out in a mild condition and does not require any special purification. This means that the process is useful and adequate for industrial mass production of 3-hydroxypyrrolidine and derivatives thereof having high optical purity.
    • 本发明涉及制备3-羟基吡咯烷或其衍生物的有效方法。 该方法包括:(a)保护4-卤代-3-羟基丁酸的羟基,(b)还原由步骤(a)得到的化合物的酯基,得到相应的醇化合物,(c)使化合物 (d)使步骤(c)中得到的化合物与胺反应,得到3-羟基保护的吡咯烷化合物,和(e)使化合物脱保护,得到3-羟基保护的吡咯烷化合物 由步骤(d)获得以产生目标3-羟基吡咯烷或其衍生物。 该方法提供了具有高光学纯度的3-羟基吡咯烷或其衍生物,因为原料的光学纯度基本保持不变。 在这个过程中,每个步骤都是在温和的条件下进行的,不需要任何特殊的纯化。 这意味着该方法对于工业大量生产具有高光学纯度的3-羟基吡咯烷及其衍生物是有用的和足够的。
    • 7. 发明申请
    • PROCESS FOR THE EFFICIENT PREPARATION OF 3-HYDROXY PYRROLIDINE AND DERIVATIVES THEREOF
    • 有效制备3-羟基吡咯烷酮及其衍生物的方法
    • WO2009011551A2
    • 2009-01-22
    • PCT/KR2008/004193
    • 2008-07-17
    • RSTECH CORPORATIONQUAN, Long GuoLEE, Jae KwanHONG, Mei HuaKIM, Kwang SubPARK, Kwang Sik
    • QUAN, Long GuoLEE, Jae KwanHONG, Mei HuaKIM, Kwang SubPARK, Kwang Sik
    • C07D207/12
    • C07D207/12
    • The present invention relates to an effective process for the preparation of 3-hydroxypyrrolidine or derivatives thereof. The process comprises (a) protecting a hydroxyl group of 4-halo-3-hydroxybutyric acid, (b) reducing an ester group of the compound obtained from the step (a) to obtain a corresponding alcohol compound, (c) reacting the compound obtained from the step (b) with sulfonyl halide to produce a corresponding sulfonate compound, (d) reacting the compound obtained from the step (c) with an amine to obtain 3-hydroxy-protected pyrrolidine compound, and (e) deprotecting the compound obtained from the step (d) to produce the targeted 3-hydroxypyrrolidine or derivatives thereof. The process provides 3-hydroxypyrrolidine or derivatives thereof with high optical purity, because optical purity of the starting material is substantially retained. In the process, each of the steps is carried out in a mild condition and does not require any special purification. This means that the process is useful and adequate for industrial mass production of 3-hydroxypyrrolidine and derivatives thereof having high optical purity.
    • 本发明涉及一种制备3-羟基吡咯烷或其衍生物的有效方法。 该方法包括(a)保护4-卤-3-羟基丁酸的羟基,(b)还原由步骤(a)获得的化合物的酯基,得到相应的醇化合物,(c)使化合物 (b)由磺酰卤获得以产生相应的磺酸盐化合物,(d)使由步骤(c)获得的化合物与胺反应,得到3-羟基保护的吡咯烷化合物,和(e)使化合物 (d)得到目标3-羟基吡咯烷或其衍生物。 该方法提供具有高光学纯度的3-羟基吡咯烷酮或其衍生物,因为起始原料的光学纯度基本保持不变。 在该过程中,每个步骤在温和条件下进行,并且不需要任何特殊的纯化。 这意味着该方法对于具有高光学纯度的3-羟基吡咯烷及其衍生物的工业批量生产是有用和充分的。
    • 8. 发明申请
    • PROCESS FOR THE PREPARATION OF HIGHLY OPTICAL PURE CARVEDILOL
    • 制备高纯度的卡维地洛的方法
    • WO2007097504A1
    • 2007-08-30
    • PCT/KR2006/003439
    • 2006-08-31
    • AHN-GOOK PHARMACEUTICAL CO., LTD.RSTECH CORPORATIONKIM, Seong-JinQUAN, Long GuoKANG, Hyun BinAUH, JinWON, Duk KwonMOON, Byung HyunJONG, Chang WooJIN, Kyung Yong
    • KIM, Seong-JinQUAN, Long GuoKANG, Hyun BinAUH, JinWON, Duk KwonMOON, Byung HyunJONG, Chang WooJIN, Kyung Yong
    • C07D209/88
    • C07D209/88C07D263/24C07D413/12Y02P20/55
    • The present invention relates to a process for the efficient preparation of highly optical pure chiral carvedilol. According to the present invention, a chiral oxazolidin-2-one or oxazolidin-2-thione having formula 2, produced from the reaction of N-protected 2-(2-methoxyphenoxy)ethylamine with a chiral glycidol derivative is used as a key intermediate for the preparation of the chiral carvedilol. Specifically, the process for the preparation of the chiral carvedilol comprises a) reacting a compound of formula 2 with a halogenation agent, a sulfonation agent or a mitsunobu reagent to activate a hydroxyl group of the compound of formula 2, followed by nucleophilic substitution reaction with 9H-4-hydroxy carbazole to produce a compound of formula 7, and b) subjecting the obtained compound of formula 7 to a deprotection reaction in a presence of an inorganic base to produce the targeted chiral carvedilol. The process of the present invention can be accomplished in a mild condition. The process neither requires any extraordinary purification procedure, nor involves decrease of optical purity. Therefore, the process of the present invention provides highly optical pure chiral carvedilol in simple and efficient manner.
    • 本发明涉及高效光学纯手性卡维地洛的高效制备方法。 根据本发明,由N-保护的2-(2-甲氧基苯氧基)乙胺与手性缩水甘醇衍生物的反应生成的具有式2的手性恶唑烷-2-酮或恶唑烷-2-硫酮用作关键中间体 用于制备手性卡维地洛。 具体地说,制备手性卡维西洛的方法包括:a)使式2的化合物与卤化剂,磺化剂或mitsunobu试剂反应以活化式2化合物的羟基,然后与 9H-4-羟基咔唑制备式7的化合物,和b)在无机碱的存在下使得到的式7的化合物进行脱保护反应,得到目标的手性卡维地洛。 本发明的方法可以在温和的条件下完成。 该方法既不需要任何非凡的纯化程序,也不涉及降低光学纯度。 因此,本发明的方法以简单有效的方式提供高光学纯手性卡维地洛。