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1. 发明申请

WO2003091267A1 PROCESS FOR PREPARING OLIGONUCLEOTIDES 审中-公开
标题翻译：制备寡核苷酸的方法
公开(公告)号：WO2003091267A1
公开(公告)日：2003-11-06
申请号：PCT/GB2003/001795
申请日：2003-04-25
申请人： AVECIA LIMITED , MOODY, David, John , WELLINGS, Donald, Alfred , McCORMAC, Paul
发明人： MOODY, David, John , WELLINGS, Donald, Alfred , McCORMAC, Paul
IPC分类号： C07H21/00
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 hydroxypolyC 2-4 alkyleneoxy chain attached to a polymerisable unit wherein the protected hydroxypolyC 2-4 alkyleneoxy chain contains from 2 to 10 C 2-4 alkyleneoxy groups and wherein the hydroxypolyC 2-4 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。

2. 发明申请

WO2003091311A1 MONOMERS CONTAINING POLYOXYALKYLENES AND POLYMER SUPPORTS THEREFROM 审中-公开
标题翻译：含有聚氧乙烯的单体和聚合物支持体
公开(公告)号：WO2003091311A1
公开(公告)日：2003-11-06
申请号：PCT/GB2003/001774
申请日：2003-04-25
申请人： AVECIA LIMITED , MOODY, David, John , WELLINGS, Donald, Alfred
发明人： MOODY, David, John , WELLINGS, Donald, Alfred
IPC分类号： C08G65/332
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 hydroxypolyC 2-4 alkyleneoxy chains attached to a cross-linked polymer wherein the protected hydroxypolyC 2-4 alkyleneoxy chain contains from 2 to 10 C 2-4 alkyleneoxy groups and wherein the hydroxypolyC 2-4 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：提供聚合物载体，其包含与交联聚合物连接的保护的羟基聚C 2-4亚烷氧基链，其中所述被保护的羟基聚C 2-4亚烷基氧基含有2至10个C 2-4亚烷基氧基，并且其中羟基聚C 2-4亚烷氧基链用酸不稳定组。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。

3. 发明申请

WO2004085454A1 SILYLATED OLIGONUCLEOTIDE COMPOUNDS 审中-公开
标题翻译：硅烷化寡核苷酸化合物
公开(公告)号：WO2004085454A1
公开(公告)日：2004-10-07
申请号：PCT/GB2004/001196
申请日：2004-03-19
申请人： AVECIA LIMITED , MOODY, David, John , MCCORMAC, Paul , BARRON, Sarah, Anne
发明人： MOODY, David, John , MCCORMAC, Paul , BARRON, Sarah, Anne
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20
摘要： Oligonucleotide comprising at least one internucleotide phosphorus atom protected with a group of formula -X a SiR 3 R 4 R 5 provided. X a represent 0 or S, and R 3 , R 4 and R 5 each independently are optionally substituted hydrocarbyl groups, selected such that that total number of carbon atoms in R 3 plus R 4 plus R 5 is 4 or more. Process for the preparation of these oligonucleotides, intermediate compounds useful therein, and process for the preparation of the intermediate compounds are also provided.
摘要翻译：提供包含至少一个被式-X-SiR 3 R 4基团保护的核苷酸间磷原子的寡核苷酸。 X a表示0或S，R 3，R 4和R 5各自独立地是任选取代的烃基，其选择为使得R 3加上R 4中的碳原子总数 >加R 5为4以上。还提供了制备这些寡核苷酸的方法，其中使用的中间体化合物和中间体化合物的制备方法。

4. 发明申请

WO2004052823A1 PROCESS FOR THE PREPARATION OF UNSATURATED ESTERS 审中-公开
标题翻译：制备不饱和酯的方法
公开(公告)号：WO2004052823A1
公开(公告)日：2004-06-24
申请号：PCT/GB2003/005332
申请日：2003-12-08
申请人： AVECIA LIMITED , MOODY, David, John , BAILEY, Mark , BARRON, Sarah, Anne
发明人： MOODY, David, John , BAILEY, Mark , BARRON, Sarah, Anne
IPC分类号： C07C67/00
CPC分类号： C07C67/313 , C07C67/343 , Y02P20/55 , C07C69/66
摘要： A process for the preparation of an unsaturated ester of Formula (1); wherein: R 1 and R 2 are each independently hydroxy protecting groups; R 3 is optionally substituted C,_ 18 alkyl; R 4 is an organic group; and R 5 is H, an organic group or R 4 and R 5 together with the C atom to which they are attached form a ring which is a component of an organic group; which comprises reacting a compound of Formula (2); wherein R 1 , R 2 and R 3 are as defined above; with an oxidising agent in the presence of a compound of formula R 4 -CHR 5 -Y wherein R 4 and R 5 are as defined above and Y represents a group forming a Wittig reagent; a P, As or Sb-containing Horner-Wadsworth Emmons reagent; a P(III), As (III) or Sb(III) precursor of a Horner-Wadsworth Emmons reagent; a Warren reagent; or a ylid precursor; and optionally a base.
摘要翻译：制备式（1）的不饱和酯的方法; 其中：R 1和R 2各自独立地为羟基保护基; R 3是任选取代的C 1-8-18烷基; R 4是有机基团; R 5为H，有机基团或R 4和R 5与它们所连接的C原子一起形成作为有机基团的组分的环; 其包括使式（2）的化合物与其中R 1，R 2和R 3如上所定义; 在式R 4 -CHR 5 -Y的化合物存在下与氧化剂反应，其中R 4和R 5如上所定义，Y代表形成Wittig试剂的基团; 一种含P，As或Sb的Horner-Wadsworth Emmons试剂; Horner-Wadsworth Emmons试剂的P（III），As（III）或Sb（III）前体; 沃伦试剂; 或前列腺素; 和任选的碱。

5. 发明申请

WO2005023737A1 PROCESS FOR THE HYDROGENATION OF ESTERS OF ALPHA-SUBSTITUTED CARBOXYLIC ACIDS 审中-公开
标题翻译：羟基取代的羧酸的加氢过程
公开(公告)号：WO2005023737A1
公开(公告)日：2005-03-17
申请号：PCT/GB2004/003884
申请日：2004-09-10
申请人： AVECIA LIMITED , MOODY, David, John , HÄRRÖD, Magnus , FIELDHOUSE, Robin
发明人： MOODY, David, John , HÄRRÖD, Magnus , FIELDHOUSE, Robin
IPC分类号： C07C29/149
CPC分类号： C07C29/149 , C07C67/31 , Y02P20/544 , C07C69/675 , C07C31/22 , C07C31/205
摘要： There is provided a process for the hydrogenation of esters of alpha-substituted carboxylic acids which comprises reacting an ester of an alpha-substituted carboxylic acid with hydrogen in the presence of a catalyst under substantially homogeneous supercritical conditions. Preferably, the ester of an alpha-substituted carboxylic acids is an ester of formula (1): wherein: R 1 and R 2 are each independently an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; and Y is a heteroatom or an optionally substituted heteroatom group. More preferably, the ester of an alpha-substituted is carboxylic acids is an ester of formula (2): wherein: R 3 is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; R 4 and R 5 are each independently hydrogen, an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; Y is a heteroatom or an optionally substituted heteroatom group; Q is a functional group; and n 1. Most preferably, the ester of an alpha-substituted carboxylic acids is an ester of formula (3): wherein: R 3 and R 6 are each independently an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; R 4 and R 5 are each independently hydrogen, an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; Y is a heteroatom or an optionally substituted heteroatom group; and n 1.
摘要翻译：提供了α-取代羧酸酯的氢化方法，其包括在催化剂存在下，在基本上均匀的超临界条件下使α-取代的羧酸的酯与氢反应。优选地，α-取代的羧酸的酯是式（1）的酯：其中：R 1和R 2各自独立地为任选取代的烃基或任选取代的杂环基; 并且Y是杂原子或任选取代的杂原子基团。更优选地，α-取代的酯是羧酸是式（2）的酯：其中：R 3是任选取代的烃基或任选取代的杂环基; R 4和R 5各自独立地为氢，任选取代的烃基或任选取代的杂环基; Y是杂原子或任选取代的杂原子基团; Q是功能组; 最优选地，α-取代的羧酸的酯是式（3）的酯：其中：R 3和R 6各自独立地是任选取代的烃基或任选取代的杂环基 ; R 4和R 5各自独立地为氢，任选取代的烃基或任选取代的杂环基; Y是杂原子或任选取代的杂原子基团; 和n 1。

6. 发明申请

WO2005012246A1 PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS, PARTICULARLY ATORVASTATIN 审中-公开
标题翻译：方法和中间体化合物在制备统计学，特别是ATORVASTATIN
公开(公告)号：WO2005012246A1
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003206
申请日：2004-07-23
申请人： AVECIA LIMITED , MOODY, David, John , WIFFEN, Jonathan, William
发明人： MOODY, David, John , WIFFEN, Jonathan, William
IPC分类号： C07D207/34
CPC分类号： C07D405/06 , C07D207/34 , C07D309/10 , C07D309/30 , Y02P20/55
摘要： There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R 1 represents a hydrogen or a hydrocarbyl group, R 2 represents a hydrogen or substituent group, R 3 represents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; P 1 represents hydrogen or a protecting group, and W represents =0 or -OP 2 , in which P 2 represents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents -OP 2 , deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents =O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof.
摘要翻译：提供了制备式（7）化合物或其盐的方法：其中R 1表示氢或烃基，R 2表示氢或取代基，R 3表示氢或烃基，X表示氢或取代基，其包含a）氰化式（1）化合物：其中Y表示卤素基团，优选Cl或Br; P 1表示氢或保护基，W表示= 0或-OP 2，其中P 2表示氢或保护基，得到式（2）的化合物：b）将式（2）化合物，得到式（3）化合物：将式（3）化合物与式（4）化合物偶合：得到式（5）化合物：当W表示-OP 2 然后氧化式（5）化合物，得到式（6）化合物：和e）当W表示= O时使式（5）的化合物或式（6）的化合物进行环 - 打开和除去任何剩余的保护基团，得到式（7）的化合物或其盐。

7. 发明申请

WO2004108633A1 PROCESS FOR THE PREPARATION OF ARYL DIAZONIUM SALTS AND REACTION WITH NUCLEOPHILES 审中-公开
标题翻译：制备二甲亚砜的制备方法和与核酸的反应
公开(公告)号：WO2004108633A1
公开(公告)日：2004-12-16
申请号：PCT/GB2004/002339
申请日：2004-06-03
申请人： AVECIA LIMITED , MOODY, David, John , HAMILL, Noel, Anthony
发明人： MOODY, David, John , HAMILL, Noel, Anthony
IPC分类号： C07B39/00
CPC分类号： C07C201/12 , C07B39/00 , C07C17/093 , C07C25/18 , C07C205/12
摘要： A process for performing nucleophilic substitution reactions on aryl diazonium salts or derivatives thereof wherein the aryl diazonium salt is first generated in an aqueous solvent system followed by partitioning of the aryl diazonium salt with a hydrophobic ionic liquid thereby allowing subsequent reaction of the aryl diazonium salt with an appropriate nucleophilic species in the hydrophobic ionic liquid to the desired product without the need to first isolate the aryl diazonium salt.
摘要翻译：在芳基重氮盐或其衍生物上进行亲核取代反应的方法，其中首先在水性溶剂体系中生成芳基重氮盐，然后用疏水性离子液体分配芳基重氮盐，从而允许芳基重氮盐与将疏水性离子液体中的适当亲核物质转化为所需产物，而无需首先分离芳基重氮盐。

8. 发明申请

WO2012020231A1 CHEMICAL LIGATION BY RING OPENING OF OXO-THIOMORPHOLINES 审中-公开
标题翻译：化学发光通过环氧化合物的开环
公开(公告)号：WO2012020231A1
公开(公告)日：2012-02-16
申请号：PCT/GB2011/001212
申请日：2011-08-12
申请人： THE UNIVERSITY OF READING , HARWOOD, Laurence, Marius , WELLINGS, Donald A , MOODY, David, John
发明人： HARWOOD, Laurence, Marius , WELLINGS, Donald A , MOODY, David, John
IPC分类号： C07K1/02 , C07K1/04
CPC分类号： C07K1/063 , C07C319/02 , C07C323/29 , C07D279/12 , C07K1/026 , C07K1/04 , C07K1/1075 , C07K5/0806 , C07K5/1008 , Y02P20/55
摘要： The invention discloses processes for preparing compounds comprising an α-amino acid motif. The compounds are useful in e.g. the chemical ligation of peptides.
摘要翻译：本发明公开了制备包含α-氨基酸基序的化合物的方法。这些化合物可用于例如肽的化学连接。

9. 发明申请

WO2006064179A1 PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS 审中-公开
标题翻译：过程和中间化合物在制备统计数据中有用
公开(公告)号：WO2006064179A1
公开(公告)日：2006-06-22
申请号：PCT/GB2005/004541
申请日：2005-11-28
申请人： AVECIA PHARMACEUTICALS LIMITED , MOODY, David, John , WIFFEN, Jonathan, William
发明人： MOODY, David, John , WIFFEN, Jonathan, William
IPC分类号： C07C51/09 , C07C61/29 , C07D209/12 , C07D215/14 , C07D257/04 , C07D309/10 , C07D405/06 , C07C69/30 , C07C67/28 , C07D209/18
CPC分类号： C07B41/08 , C07C51/09 , C07D209/24 , C07D215/14 , C07D257/04 , C07D309/10 , C07D309/30 , C07D405/06 , Y02P20/55 , C07C59/58
摘要： There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein R a represents an alkyl group, such as a C 1-16 alkyl group, and preferably an isopropyl group; R b represents an aryl group, preferably a 4-fluorophenyl group; R c represents hydrogen, a protecting group or an alkyl group, such as a C 1-16 alkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SO 2 R e group where R e is an alkyl group, such as a C 1 - 16 alkyl group, and preferably a methyl group.
摘要翻译：提供制备式（7）化合物的方法：其中R是任选取代的烃基或任选取代的杂环基; 提供R不是式（a）的化合物：其中R a a表示烷基，例如C 1-16烷基，优选异丙基 ; R b表示芳基，优选4-氟苯基; R c表示氢，保护基或烷基，例如C 1-16烷基，优选甲基; 并且Rd表示氢，保护基或SO 2 R e基团，其中R e是烷基，例如C

10. 发明申请

WO2005092867A3 PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS, PARTICULARLY ROSUVASTATIN 审中-公开
公开(公告)号：WO2005092867A3
公开(公告)日：2005-10-06
申请号：PCT/GB2005/001099
申请日：2005-03-23
申请人： AVECIA PHARMACEUTICALS LIMITED , MOODY, David, John , WIFFEN, Jonathan, William
发明人： MOODY, David, John , WIFFEN, Jonathan, William
IPC分类号： A61K31/505
摘要： There is provided a process for the preparation of a compound of formula (7) wherein R 1 represents an alkyl group; R 2 represents an aryl group; R 3 represents hydrogen, a protecting group or an alkyl group; and R 4 represents hydrogen, a protecting group or a SO 2 R 5 group where R 5 is an alkyl group, which comprises a) hydroxylating a compound of formula (1) wherein Y represents a halo group; P 1 represents hydrogen or a protecting group, and W represents =O or -OP 2 , in which P 2 represents hydrogen or a protecting group, to give a compound of formula (2), b) oxidising the compound of formula (2) to give a compound of formula (3), c) coupling the compound of formula (3) with a compound of formula (4), wherein R 3 represents a protecting group or an alkyl group; R 4 represents a protecting group or a SO 2 R 5 group where R 5 is an alkyl group; and R 6 represents (PR 7 R 8 ) + X - or P(=O)R 7 R 8 in which X is an anion and R 7 and R 8 each independently is an alkyl, aryl.

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