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1. 发明授权

US08093397B2 Activators for oligonucleotide synthesis 有权
标题翻译：寡核苷酸合成活化剂
公开(公告)号：US08093397B2
公开(公告)日：2012-01-10
申请号：US12287116
申请日：2008-10-06
申请人： Nanda Sinha , William Edward Zedalis , Gregory Keith Miranda
发明人： Nanda Sinha , William Edward Zedalis , Gregory Keith Miranda
IPC分类号： C07D275/06
CPC分类号： C07D275/06 , C07D213/18 , C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586 , C07F9/65616 , C07H21/00 , C07H21/04
摘要： A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one is represented by the following structural formula: wherein p is 0 or an integer from 1 to 4; X7 is O or S; R for each occurrence is a substituent, preferably each independently, a halo, a substituted or unsubstituted aliphatic group, —NR11R12, —OR13, —OC(O)R13, —C(O)OR13, or cyano; or two adjacent R groups taken together with the carbon atoms to which they are attached form a six membered saturated or unsaturated ring; R11 and R12 are each, independently, —H, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and R13 is a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group. Preferred organic bases are pyridine, 3-methylpyridine, or N-methylimidazole.
摘要翻译：提供了使用亚磷酰胺化学合成寡核苷酸的方法。该方法优选在有机碱的存在下使用1,1-二氧代-1,2-二氢-1λ6-苯并[d]异噻唑-3-酮作为活化剂。 1,1-二氧代-1,2-二氢-1λ6-苯并[d]异噻唑-3-酮由以下结构式表示：其中p为0或1至4的整数; X7为O或S; 每个出现的R是取代基，优选各自独立地是卤素，取代或未取代的脂族基，-NR 11 R 12，-OR 13，-OC（O）R 13，-C（O）OR 13或氰基; 或两个相邻的R基团与它们所连接的碳原子一起形成六元饱和或不饱和环; R 11和R 12各自独立地为-H，取代或未取代的脂族基团，取代或未取代的芳基或取代或未取代的芳烷基; R 13为取代或未取代的脂族基团，取代或未取代的芳基或取代或未取代的芳烷基。优选的有机碱是吡啶，3-甲基吡啶或N-甲基咪唑。

2. 发明授权

US07872121B2 Process for the removal of exocyclic base protecting groups 有权
标题翻译：去除环外基保护基团的方法
公开(公告)号：US07872121B2
公开(公告)日：2011-01-18
申请号：US11578961
申请日：2005-04-15
申请人： Nanda Dulal Sinha , Satya Kuchimanchi
发明人： Nanda Dulal Sinha , Satya Kuchimanchi
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , Y02P20/55
摘要： Nitrogen-protecting groups are removed from the exocyclic nucleobase portion of a 2′-O protected nucleotide or 2′-halo nucleotide by contacting the nucleotide with an inorganic base. Typical is the removal of t-butylphenoxyacetyl protecting groups from the nucleobase portion of a 2′-O protected nucleotide on which the 2′-O protecting group is t-butyldimethylsilyl, removal or deprotection being accomplished by contact with a potassium carbonate solution.
摘要翻译：通过使核苷酸与无机碱接触，从2'-O保护的核苷酸或2'-卤代核苷酸的环外核碱基部分除去氮保护基团。典型的是从2'-O保护基团是叔丁基二甲基甲硅烷基的2'-O保护的核苷酸的核碱基部分除去叔丁基苯氧基乙酰基保护基，通过与碳酸钾溶液接触来除去或去保护。

3. 发明申请

US20020072593A1 Method of preventing modification of synthetic oligonucleotides 失效
标题翻译：防止合成寡核苷酸修饰的方法
公开(公告)号：US20020072593A1
公开(公告)日：2002-06-13
申请号：US09879859
申请日：2001-06-12
申请人： Avecia Biotechnology Inc.
发明人： Nanda D. Sinha
IPC分类号： C07H021/04
CPC分类号： C07H21/00 , C07H1/06 , Y02P20/55
摘要： The present invention relates to a method of preventing modification of a synthetic oligonucleotide or oligonucleotide analog during removal of at least one null-cyanoethyl protecting group from the oligonucleotide or oligonucleotide analog. The method involves contacting the oligonucleotide or oligonucleotide analog with a basic solution having at least one acrylonitrile scavenger, such as t-butylamine, at a sufficient temperature and for a sufficient period of time to remove at least one null-cyanoethyl protecting group. The present invention also relates to a method of producing a synthetic oligonucleotide or oligonucleotide analog.
摘要翻译：本发明涉及在从寡核苷酸或寡核苷酸类似物中除去至少一个β-氰基乙基保护基团时，防止合成寡核苷酸或寡核苷酸类似物的修饰的方法。该方法包括使寡核苷酸或寡核苷酸类似物与具有至少一种丙烯腈清除剂如叔丁胺的碱性溶液在足够的温度下接触足够的时间以除去至少一个β-氰乙基保护基。本发明还涉及合成寡核苷酸或寡核苷酸类似物的制备方法。

4. 发明授权

US07501505B2 Activators for oligonucleotide synthesis 有权
标题翻译：寡核苷酸合成活化剂
公开(公告)号：US07501505B2
公开(公告)日：2009-03-10
申请号：US10482441
申请日：2002-07-01
申请人： Nanda Sinha , William Edward Zedalis , Gregory Keith Miranda
发明人： Nanda Sinha , William Edward Zedalis , Gregory Keith Miranda
IPC分类号： C07H21/02 , C07H21/04 , C07D275/06
CPC分类号： C07D275/06 , C07D213/18 , C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586 , C07F9/65616 , C07H21/00 , C07H21/04
摘要： A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one is represented by the following structural formula: wherein p is 0 or an integer from 1 to 4; X7 is O or S; R for each occurrence is a substituent, preferably each independently, a halo, a substituted or unsubstituted aliphatic group, —NR11R12, —OR13, —OC(O)R13, —C(O)OR13, or cyano; or two adjacent R groups taken together with the carbon atoms to which they are attached form a six membered saturated or unsaturated ring; R11 and R12 are each, independently, —H, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and R13 is a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group. Preferred organic bases are pyridine, 3-methylpyridine, or N-methylimidazole.
摘要翻译：提供了使用亚磷酰胺化学合成寡核苷酸的方法。该方法优选在有机碱的存在下使用1,1-二氧代-1,2-二氢-1λ6-苯并[d]异噻唑-3-酮作为活化剂。 1,1-二氧代-1,2-二氢-1λ6-苯并[d]异噻唑-3-酮由以下结构式表示：其中p为0或1至4的整数; X7为O或S; 每个出现的R是取代基，优选各自独立地是卤素，取代或未取代的脂族基，-NR 11 R 12，-OR 13，-OC（O）R 13，-C（O）OR 13或氰基; 或两个相邻的R基团与它们所连接的碳原子一起形成六元饱和或不饱和环; R 11和R 12各自独立地为-H，取代或未取代的脂族基团，取代或未取代的芳基或取代或未取代的芳烷基; R 13为取代或未取代的脂族基团，取代或未取代的芳基或取代或未取代的芳烷基。优选的有机碱是吡啶，3-甲基吡啶或N-甲基咪唑。

5. 发明授权

US07247720B2 Phosphitylation process 有权
标题翻译：磷化过程
公开(公告)号：US07247720B2
公开(公告)日：2007-07-24
申请号：US10531323
申请日：2003-10-08
申请人： Nanda Dulal Sinha
发明人： Nanda Dulal Sinha
IPC分类号： C07H21/00 , C07H19/04
CPC分类号： C07H19/06 , C07F9/24 , C07H19/04 , C07H19/16 , C07H21/00
摘要： A process for the phosphitylation of an alcohol or thiol with a phosphitylation agent in the presence of an activator is provided. The activator has the formula: wherein p is 0 or an integer from 1 to 4 and R for each occurrence is a substituent. Preferably X7 is O and p is 0. The activator is commonly employed as a salt complex with an organic base. Preferred alcohols or thiols include nucleosides and oligonucleotides. The process is particularly suited for the synthesis of phosphoramidites.
摘要翻译：提供了在活化剂存在下使醇或硫醇与磷酸化剂磷酸化的方法。活化剂具有下式：其中p为0或1至4的整数，R为每次出现时为取代基。优选地，X 7是O，p是0.通常使用活化剂作为与有机碱的盐络合物。优选的醇或硫醇包括核苷和寡核苷酸。该方法特别适用于亚磷酰胺的合成。

6. 发明申请

US20060069247A1 Phosphitylation process 有权
标题翻译：磷化过程
公开(公告)号：US20060069247A1
公开(公告)日：2006-03-30
申请号：US10531323
申请日：2003-10-08
申请人： Nanda Sinha
发明人： Nanda Sinha
IPC分类号： C07H19/04 , C07H21/00
CPC分类号： C07H19/06 , C07F9/24 , C07H19/04 , C07H19/16 , C07H21/00
摘要： A process for the phosphitylation of an alcohol or thiol with a phosphitylation agent in the presence of an activator is provided. The activator has the formula: wherein p is 0 or an integer from 1 to 4 and R for each occurrence is a substituent. Preferably X7 is O and p is 0. The activator is commonly employed as a salt complex with an organic base. Preferred alcohols or thiols include nucleosides and oligonucleotides. The process is particularly suited for the synthesis of phosphoramidites.
摘要翻译：提供了在活化剂存在下使醇或硫醇与磷酸化剂磷酸化的方法。活化剂具有下式：

7. 发明授权

US07560555B2 Process for the preparation of phosphitylation agents 有权
标题翻译：磷酸化剂的制备方法
公开(公告)号：US07560555B2
公开(公告)日：2009-07-14
申请号：US10539210
申请日：2003-12-16
申请人： Jonathan Mark Hardy , Stephen Edward Dinizo
发明人： Jonathan Mark Hardy , Stephen Edward Dinizo
IPC分类号： C07F9/52
CPC分类号： C07F9/26 , C07F9/2408 , Y02P20/55
摘要： A process for the preparation of a compound of formula R1—Y1—P(NR2R3)2 is provided. The process comprises reacting a compound of formula PX3 with a compound of formula HNR2R3 to form a compound of formula X—P(NR2R3)2; and reacting the compound of formula X—P(NR2R3)2 with a compound of formula R1—Y1—H in the presence of a hydrocarbon solvent to form the compound of formula R1—Y1—P(NR2R3)2. R1 represents a phosphorus protecting group; R2 and R3 each independently represent an alkyl, prefer-ably a C1-6alkyl, group, or R2 and R3 are joined, together with the N to which they are attached, to form a 5-7 membered ring; Y1 represents O or S, preferably O; and X represents a halogen, preferably Cl. The preferred solvent is toluene.
摘要翻译：提供了制备式R1-Y1-P（NR2R3）2化合物的方法。该方法包括使式PX3的化合物与式HNR 2 R 3的化合物反应以形成式X-P（NR 2 R 3）2的化合物; 并在烃溶剂存在下使式X-P（NR 2 R 3）2化合物与式R1-Y1-H化合物反应，形成式R 1 -Y 1 -P（NR 2 R 3）2化合物。 R1表示磷保护基; R 2和R 3各自独立地表示烷基，优选C 1-6烷基，或者R 2和R 3与它们所连接的N一起连接形成5-7元环; Y1表示O或S，优选O; X表示卤素，优选Cl。优选的溶剂是甲苯。

8. 发明申请

US20090085006A1 Activators for oligonucleotide synthesis 有权
公开(公告)号：US20090085006A1
公开(公告)日：2009-04-02
申请号：US12287116
申请日：2008-10-06
申请人： Nanda Sinha , William Edward Zedalis , Gregory Keith Miranda
发明人： Nanda Sinha , William Edward Zedalis , Gregory Keith Miranda
IPC分类号： C09K3/00 , C07D275/06
CPC分类号： C07D275/06 , C07D213/18 , C07D231/12 , C07D233/56 , C07D249/08 , C07F9/65586 , C07F9/65616 , C07H21/00 , C07H21/04
摘要： A process for the synthesis of oligonucleotides using phosphoramidite chemistry is provided. The process employs as activator a 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one, preferably in the presence of an organic base. The 1,1-dioxo-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one is represented by the following structural formula: wherein p is 0 or an integer from 1 to 4; X7 is O or S; R for each occurrence is a substituent, preferably each independently, a halo, a substituted or unsubstituted aliphatic group, —NR11R12, —OR13, —OC(O)R13, —C(O)OR13, or cyano; or two adjacent R groups taken together with the carbon atoms to which they are attached form a six membered saturated or unsaturated ring; R11 and R12 are each, independently, —H, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group; and R13 is a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aralkyl group. Preferred organic bases are pyridine, 3-methylpyridine, or N-methylimidazole.

9. 发明授权

US07476709B2 Process for preparing oligonucleotides 有权
标题翻译：寡核苷酸的制备方法
公开(公告)号：US07476709B2
公开(公告)日：2009-01-13
申请号：US10512138
申请日：2003-04-25
申请人： David John Moody , Donald Alfred Wellings , Paul McCormac
发明人： David John Moody , Donald Alfred Wellings , Paul McCormac
IPC分类号： C08F16/12 , C08F8/12
CPC分类号： C07H21/00 , C08F12/22 , C08F290/00 , C08F290/06 , C08F290/062 , C08G65/329 , C08G65/3326 , C08L71/02 , C08L2205/05 , Y02P20/55 , C08L2666/04
摘要： A process for the preparation of an oligonucleotide is provided. The process comprises the assembly of an oligonucleotide attached to a solid support, wherein the solid support is prepared by a process comprising polymerisation of a monomer which comprises a protected hydroxypolyC2-4 alkyleneoxy chain attached to a polymerisable unit wherein the protected hydroxypolyC2-4 alkyleneoxy chain contains from 2 to 10 C2-4 alkyleneoxy groups and wherein the hydroxypolyC2-4 alkyleneoxy chain is protected with an acid-labile protecting group, preferably an optionally substituted trityl group.
摘要翻译：提供了制备寡核苷酸的方法。该方法包括连接到固体支持物上的寡核苷酸的组装，其中固体支持物通过包含聚合单体的方法制备，所述方法包括连接于可聚合单元上的被保护的羟基聚C 2-4亚烷氧基链，其中所述保护的羟基聚C 2-4亚烷基氧基链含有2至10个C 2-4亚烷氧基并且其中羟基聚C 2-4亚烷氧基链用酸不稳定保护基保护，优选任选取代的三苯甲基。

10. 发明授权

US07365132B2 Monomers containing polyoxyalkylenes and polymer supports therefrom 有权
标题翻译：含有聚氧化烯的单体和其聚合物载体
公开(公告)号：US07365132B2
公开(公告)日：2008-04-29
申请号：US10512145
申请日：2003-04-25
申请人： David John Moody , Donald Alfred Wellings
发明人： David John Moody , Donald Alfred Wellings
IPC分类号： C08F16/12 , C07C43/215
CPC分类号： C07H21/00 , C08F12/22 , C08F290/00 , C08F290/06 , C08F290/062 , C08G65/329 , C08G65/3326 , C08L71/02 , C08L2205/05 , Y02P20/55 , C08L2666/04
摘要： A polymer support is provided which comprises protected hydroxypolyC2-4 alkyleneoxy chains attached to a cross-linked polymer wherein the protected hydroxypolyC2-4 alkyleneoxy chain contains from 2 to 10 C2-4 alkyleneoxy groups and wherein the hydroxypolyC2-4 alkyleneoxy chains are protected with an acid labile group. The acid labile protecting group is preferably a poly-aryl methane protecting group. A monomer and process for the preparation of said support are also provided.
摘要翻译：提供了一种聚合物载体，其包含与交联聚合物连接的保护的羟基聚二醇2-4亚烷氧基链，其中保护的羟基聚二醇亚烷基氧基链含有2至10个碳原子 2-4个亚烷基氧基，其中羟基聚C 2-4亚烷氧基链用酸不稳定基团保护。酸不稳定保护基优选为聚芳基甲烷保护基。还提供了用于制备所述载体的单体和方法。

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