公开(公告)号：US20100273999A1

公开(公告)日：2010-10-28

申请号：US12775843

申请日：2010-05-07

申请人： Kyeong-Eun Jung ,  Alexei Kayushin ,  Moon Hee Kim ,  Kyung-Il Kim ,  Sungwon Kim ,  Yumi Ji

发明人： Kyeong-Eun Jung ,  Alexei Kayushin ,  Moon Hee Kim ,  Kyung-Il Kim ,  Sungwon Kim ,  Yumi Ji

IPC分类号： C07H1/00 ,  C07H21/00

CPC分类号： C07H21/02 ,  C07H1/00 ,  C07H19/067 ,  C07H19/10 ,  C07H19/167 ,  C07H19/20

摘要： The present invention provides a method for preparing nucleotide oligomers, including (a) coupling a nucleotide dimer or nucleotide trimer to a nucleoside attached to solid supports or to universal solid supports as a starting material; (b) sequentially coupling nucleotide monomers to the resulting structures of Step (a) to prepare a nucleotide oligomer; and (c) removing the nucleotide oligomers from the solid supports.The method of the present invention provides nucleotide oligomers having 15-20% higher purity than the conventional art. The present invention enables the efficient and inexpensive synthesis of nucleotide oligomers with high purity within a shorter period of time.

摘要翻译： 本发明提供了制备核苷酸寡聚体的方法，包括（a）将核苷酸二聚体或核苷酸三聚体与连接至固体支持物的核苷或作为起始材料的通用固体支持物偶联; （b）顺序地将核苷酸单体与步骤（a）的所得结构偶联以制备核苷酸寡聚物; 和（c）从固体支持物中除去核苷酸寡聚体。 本发明的方法提供了具有比常规技术高15-20％的核苷酸寡聚物。 本发明能够在更短的时间内高效且廉价地合成具有高纯度的核苷酸低聚物。

公开(公告)号：US20090292117A1

公开(公告)日：2009-11-26

申请号：US12312889

申请日：2007-10-24

申请人： Kyung-ll Kim ,  Seung-Bum Ha ,  Jae-Hoon Jeon ,  Soon-Jeong Kwon ,  Yong-Tae Kim ,  Ji-Suk Yun

发明人： Kyung-ll Kim ,  Seung-Bum Ha ,  Jae-Hoon Jeon ,  Soon-Jeong Kwon ,  Yong-Tae Kim ,  Ji-Suk Yun

IPC分类号： C07H3/02

CPC分类号： C07H3/02

摘要： A method of preparing 2-deoxy-L-ribose represented by the following formula I is disclosed. The preparation method includes the steps of: treating L-arabinose with an alcohol solvent in the presence of an acid to prepare 1-alkoxy-L-arabinopyranose; allowing the prepared 1-alkoxy-L-arabinopyranose to react with acyl chloride so as to prepare 1-alkoxy-2,3,4-triacyl-L-arabinopyranose; brominating the alkoxy group of the prepared 1-alkoxy-2,3,4-triacyl-L-arabinopyranose to prepare a 1-bromo-2,3,4-triacyl compound; allowing the prepared compound to react with zinc in the presence of ethyl acetate and an organic base so as to prepare glycal; treating the glycal with an alcohol solvent in the presence of an acid to prepare 1-alkoxy-2-deoxy-3,4-diacyl-L-ribopyranose; treating the prepared 1-alkoxy-2-deoxy-3,4-diacyl-L-ribopyranose with a base to prepare 1-alkoxy-2-deoxy-L-ribopyranose; and hydrolyzing the prepared 1-alkoxy-2-deoxy-L-ribopyranose in the presence of an acid catalyst.

摘要翻译： 公开了制备由下式I表示的2-脱氧-L-核糖的方法。 该制备方法包括以下步骤：在酸存在下用醇溶剂处理L-阿拉伯糖以制备1-烷氧基-L-阿拉伯吡喃糖; 使制备的1-烷氧基-L-阿拉伯吡喃与酰氯反应，制得1-烷氧基-2,3,4-三酰基-L-阿拉伯吡喃糖; 溴化制备的1-烷氧基-2,3,4-三酰基-L-阿拉伯吡喃糖的烷氧基以制备1-溴-2,3,4-三酰基化合物; 使得制备的化合物在乙酸乙酯和有机碱的存在下与锌反应，以制备甘氨酸; 在酸的存在下用醇溶剂处理甘氨酸以制备1-烷氧基-2-脱氧-3,4-二酰基-L-吡喃糖; 用碱处理制备的1-烷氧基-2-脱氧-3,4-二酰基-L-吡喃糖，制备1-烷氧基-2-脱氧-L-吡喃糖; 并在酸催化剂存在下水解制备的1-烷氧基-2-脱氧-L-吡喃糖。

公开(公告)号：US07304154B2

公开(公告)日：2007-12-04

申请号：US10521022

申请日：2003-07-15

申请人： Jae-Sung Kang ,  Mi-Hong Yun ,  Sang-Dae Lee ,  Byoung-Chan Jeon ,  Jeong-Ah Shin

发明人： Jae-Sung Kang ,  Mi-Hong Yun ,  Sang-Dae Lee ,  Byoung-Chan Jeon ,  Jeong-Ah Shin

IPC分类号： C07H3/08 ,  C07H3/02

CPC分类号： C07H3/08 ,  C07H1/00 ,  C07H3/02

摘要： The present invention relates to an economic synthetic method of 2-deoxy-L-ribose with easy reaction, separation and purification. The present invention consists of four (4) steps including protection, activation of 3- and 4-OH groups, inversion and deprotection steps. In respect to the cost for equipment, reagent and operation, by the present invention, 2-deoxy-L-ribose can be produced more economically because the invention uses 2-deoxy-L-ribose which is abundant in nature and easily synthesized from D-glucose and adopt simple and yielding process.

摘要翻译： 本发明涉及2-脱氧-L-核糖的经济合成方法，其易于反应，分离和纯化。 本发明包括四（4）步骤，包括保护，活化3-和4-羟基，反转和脱保护步骤。 关于设备，试剂和操作的成本，通过本发明，可以更经济地制备2-脱氧L-核糖，因为本发明使用自然界丰富且易于从D合成的2-脱氧-L-核糖 - 葡萄糖并采用简单和屈服过程。

公开(公告)号：US20060263859A1

公开(公告)日：2006-11-23

申请号：US11412452

申请日：2006-04-27

申请人： Dong Seong ,  Se Han ,  Seong Song ,  Byoung Hahm ,  Soo Rhie ,  Jae Kang

发明人： Dong Seong ,  Se Han ,  Seong Song ,  Byoung Hahm ,  Soo Rhie ,  Jae Kang

IPC分类号： C12P19/30 ,  C07H19/00

CPC分类号： C12P19/32

摘要： Disclosed therein is a method for preparing the 3′-amino-2′,3′-dideoxyguanosine, comprising the steps of: (a) treating 3′-amino-3′-deoxythymidine and 2,6-diaminopurine with a pyrimidine nucleoside phosphorylase and a purine nucleoside phosphorylase to prepare 3′-amino-2′,3′-dideoxyribosyl 2,6-diaminopurine; and (b) converting enzymatically the 3′-amino-2′,3′-dideoxyribosyl 2,6-diaminopurine with an adenosine deaminase to prepare 3′-amino-2′,3′-dideoxyguanosine. According to the present invention, 3′-amino-2′,3′-dideoxyguanosine may be obtained with very high yield in a relatively simple procedure.

摘要翻译： 其中公开了一种制备3'-氨基-2'，3'-二脱氧鸟苷的方法，包括以下步骤：（a）用嘧啶核苷磷酸化酶处理3'-氨基-3'-脱氧胸苷和2,6-二氨基嘌呤 和嘌呤核苷磷酸化酶，制备3'-氨基-2'，3'-二脱氧核糖基2,6-二氨基嘌呤; 和（b）用腺苷脱氨酶酶解3'-氨基-2'，3'-二脱氧核糖基2,6-二氨基嘌呤以制备3'-氨基-2'，3'-二脱氧鸟苷。 根据本发明，可以以相对简单的方法以非常高的产率获得3'-氨基-2'，3'-二脱氧鸟苷。

公开(公告)号：US08114987B2

公开(公告)日：2012-02-14

申请号：US12312889

申请日：2007-10-24

申请人： Kyung-Il Kim ,  Seung-Bum Ha ,  Jae-Hoon Jeon ,  Soon-Jeong Kwon ,  Yong-Tae Kim ,  Ji-Suk Yun

发明人： Kyung-Il Kim ,  Seung-Bum Ha ,  Jae-Hoon Jeon ,  Soon-Jeong Kwon ,  Yong-Tae Kim ,  Ji-Suk Yun

IPC分类号： C07H15/00 ,  C07H17/00 ,  C07H1/00 ,  C07H3/00 ,  C07G3/00 ,  C08B37/00

CPC分类号： C07H3/02

摘要： A method of preparing 2-deoxy-L-ribose represented by the following formula I is disclosed. The preparation method includes the steps of: treating L-arabinose with an alcohol solvent in the presence of an acid to prepare 1-alkoxy-L-arabinopyranose; allowing the prepared 1-alkoxy-L-arabinopyranose to react with acyl chloride so as to prepare 1-alkoxy-2,3,4-triacyl-L-arabinopyranose; brominating the alkoxy group of the prepared 1-alkoxy-2,3,4-triacyl-L-arabinopyranose to prepare a 1-bromo-2,3,4-triacyl compound; allowing the prepared compound to react with zinc in the presence of ethyl acetate and an organic base so as to prepare glycal; treating the glycal with an alcohol solvent in the presence of an acid to prepare 1-alkoxy-2-deoxy-3,4-diacyl-L-ribopyranose; treating the prepared 1-alkoxy-2-deoxy-3,4-diacyl-L-ribopyranose with a base to prepare 1-alkoxy-2-deoxy-L-ribopyranose; and hydrolyzing the prepared 1-alkoxy-2-deoxy-L-ribopyranose in the presence of an acid catalyst.

摘要翻译： 公开了制备由下式I表示的2-脱氧-L-核糖的方法。 该制备方法包括以下步骤：在酸存在下用醇溶剂处理L-阿拉伯糖以制备1-烷氧基-L-阿拉伯吡喃糖; 使制备的1-烷氧基-L-阿拉伯吡喃与酰氯反应，制得1-烷氧基-2,3,4-三酰基-L-阿拉伯吡喃糖; 溴化制备的1-烷氧基-2,3,4-三酰基-L-阿拉伯吡喃糖的烷氧基以制备1-溴-2,3,4-三酰基化合物; 使得制备的化合物在乙酸乙酯和有机碱的存在下与锌反应，以制备甘氨酸; 在酸的存在下用醇溶剂处理甘氨酸以制备1-烷氧基-2-脱氧-3,4-二酰基-L-吡喃糖; 用碱处理制备的1-烷氧基-2-脱氧-3,4-二酰基-L-吡喃糖，制备1-烷氧基-2-脱氧-L-吡喃糖; 并在酸催化剂存在下水解制备的1-烷氧基-2-脱氧-L-吡喃糖。

公开(公告)号：US20060167277A1

公开(公告)日：2006-07-27

申请号：US11388883

申请日：2006-03-24

申请人： Jae-Sung Kang ,  Sun-Ki Chang ,  Kyoung-Mee Seol ,  Min-Kyu Kim

发明人： Jae-Sung Kang ,  Sun-Ki Chang ,  Kyoung-Mee Seol ,  Min-Kyu Kim

IPC分类号： C07D405/02

CPC分类号： C07D405/04 ,  Y02P20/55

摘要： The present invention relates to new aziridine derivative that is represented by following general chemical formulae (la) or (lb), and to their preparation method. In the above mentioned chemical formulae, R2 and R3 can be same or different, and they are hydrogen, low-quality alkyl or cycloalkyl respectively; R4 can be selected among hydrogen, alkyl, aril, or amino protective group, and amino protective group is, for example, (PH)3C, FMOC (9-fluorenylmethyl oxycarbonyl), alkoxycarbonyl, ariloxycarbonyl, aralkyloxycarbonyl and R5CO, R5SO2 where R5 is alkyl or aril or aralkyl.

摘要翻译： 本发明涉及由以下一般化学式（Ia）或（Ib）表示的新的氮丙啶衍生物及其制备方法。 在上述化学式中，R 2和R 3可以相同或不同，它们分别是氢，低质量烷基或环烷基; R 4可以选自氢，烷基，芳基或氨基保护基，氨基保护基是例如（PH）3 C，FMOC（9- 芴基甲基氧羰基），烷氧基羰基，芳氧基羰基，芳烷氧基羰基和R 5 CO，R 5 SO 2，其中R 5是 烷基或芳基或芳烷基。

公开(公告)号：US07049447B2

公开(公告)日：2006-05-23

申请号：US10473259

申请日：2002-04-19

申请人： Jae-Sung Kang ,  Sun-Ki Chang ,  Kyoung-Mee Seol ,  Min-Kyu Kim

发明人： Jae-Sung Kang ,  Sun-Ki Chang ,  Kyoung-Mee Seol ,  Min-Kyu Kim

IPC分类号： C07D405/04

CPC分类号： C07D405/04 ,  Y02P20/55

摘要： The present invention relates to a new aziridine derivative that is represented herein by general chemical formulae (Ia) or (Ib), and to their preparation method. In the said chemical formulae, R2 and R3 can be the same or different, and they are hydrogen, low-quality alkyl or cycloalkyl respectively; R4 can be selected among hydrogen, alkyl, aryl, or amino protective group; and amino protective group is, for example, (Ph)3C, and FMOC(9-fluorenylmethyloxycarbonyl), alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl and R5CO, R5SO2 where R5 is alkyl, aryl or aralkyl.

摘要翻译： 本发明涉及一般化学式（Ia）或（Ib）表示的新的氮丙啶衍生物及其制备方法。 在所述化学式中，R 2和R 3可以相同或不同，它们分别是氢，低质量烷基或环烷基; R 4可以选自氢，烷基，芳基或氨基保护基; 和氨基保护基是例如（Ph）3 C，和FMOC（9-芴基甲氧基羰基），烷氧基羰基，芳氧基羰基，芳烷氧基羰基和R 5 CO，R SUB 芳基或芳烷基，其中R 5是烷基，芳基或芳烷基。