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1. 发明申请

WO2005123971A2 SCAVENGER SUPPORTS AND THE USE THEREOF IN A PROCESS FOR THE EXTRACTION OF METALS 审中-公开
标题翻译： SCAVENGER支持与AMINO功能的助剂KETOESTER或KETOMIDE组合从解决方案中移除金属
公开(公告)号：WO2005123971A2
公开(公告)日：2005-12-29
申请号：PCT/GB2005/002308
申请日：2005-06-13
申请人： AVECIA PHARMACEUTICALS LIMITED , PEARS, David, Alan , TREACHER, Kevin, Edward
发明人： PEARS, David, Alan , TREACHER, Kevin, Edward
IPC分类号： C22B3/24
CPC分类号： C22B3/24 , B01J20/02 , B01J20/26 , B01J20/265 , B01J20/267 , B01J20/32 , B01J20/3204 , B01J20/3208 , B01J20/3242 , B01J20/3244 , B01J20/3251 , B01J20/3253 , B01J20/3255 , B01J45/00 , C22B11/048 , Y02P10/214 , Y02P10/234 , Y02W30/54
摘要： There is provided a process for removing metal from solution wherein a solution comprising a metal is contacted with a scavenger support, whereby the scavenger support binds to at least some of the metal in solution thereby decreasing the amount of metal in solution, characterised in that the scavenger support comprises a functionalised support comprising pendant groups selected from 1,3-ketoesters or 1,3-ketoamides or mixtures thereof attached to a support wherein a number of the pendant groups are reacted with an amine. Scavenger supports comprising a functionalised support comprising pendant 1,3ketoester or 1,3-ketoamide groups of formula 1: wherein R 1 is an optionally substituted hydrocarbyl, perhalogenated hydrocarbyl or heterocyclyl group; X is O or NR 2 , wherein the free valence of O or NR 2 is bonded to a support optionallly via a linker; and R 2 is hydrogen, an optionally substituted hydrocarbyl, or heterocyclyl group, wherein a number of the pendant groups are reacted with an amine are also provided. Preferred scavenger supports include scavenger supports comprising pendant 3-iminoesters, 3-iminoamides, 2,3-enaminoesters or 2,3-enaminoamides pendant groups of Formula (3) or (4): wherein R 1 is an optionally substituted hydrocarbyl, perhalogenated hydrocarbyl or heterocyclyl group; X is O or NR 2 , wherein the free valence of O or NR 2 is bonded to a support optionally via a linker; R 2 is hydrogen, an optionally substituted hydrocarbyl, or heterocyclyl group; R 4 is a substituent group; and R 5 is hydrogen or a substituent group, or R 4 and R 5 may optionally be linked in such a way so as to form an optionally substituted heterocyclic ring, or tautomers or salts thereof.
摘要翻译：提供了一种从溶液中除去金属的方法，其中包含金属的溶液与清除剂载体接触，由此清除剂载体与溶液中的至少一些金属结合，从而减少溶液中的金属的量，其特征在于，清除剂载体包含官能化载体，其包含选自1,3-酮酯或1,3-酮酰胺或其混合物的侧基，其连接到载体上，其中许多侧基与胺反应。清除剂载体包含官能化载体，其包含式（1）的1,3-酮酯或1,3-酮酰胺基团：其中R 1是任选取代的烃基，全卤代烃基或杂环基; X是O或NR 2，其中O或NR 2的游离价键可以通过连接体选择性地键合到支持物上; 并且还提供了其中许多侧基与胺反应的R 2是氢，任选取代的烃基或杂环基。优选的清除剂载体包括清除剂载体，其包含3-聚亚胺酯侧链，3-亚氨基酰胺，2,3-烯氨基酯或连接到聚合物载体上的2,3-烯氨基酰胺侧基。或者，清除剂载体是可从氨基官能化硅胶获得的官能化无机载体。从与清除剂载体接触的溶液中除去的金属优选为过渡金属，更优选铂族金属如钯。

2. 发明申请

WO2005108346A1 PROCESS FOR THE PREPARATION OF ALLYLIC AMINES 审中-公开
标题翻译：制备多种氨基酸的方法
公开(公告)号：WO2005108346A1
公开(公告)日：2005-11-17
申请号：PCT/GB2005/001693
申请日：2005-05-06
申请人： AVECIA PHARMACEUTICALS LIMITED , BLACKER, Andrew, John , VEIGHEY, Clifford, Robert , MURRAY, Ernest, Jonathan , ATHERTON, John, Heathcote
发明人： BLACKER, Andrew, John , VEIGHEY, Clifford, Robert , MURRAY, Ernest, Jonathan , ATHERTON, John, Heathcote
IPC分类号： C07C209/14
CPC分类号： C07C209/70 , C07C209/16 , C07C211/21
摘要： There is provided a process for the preparation of an allylic amine formula (IV): formula (IV) which comprises a) reacting an alkynol of formula (I) : formula (I) with an activating agent to give an activated alkynol of formula (II): formula (II) OR 3 is a leaving group, b) reacting the activated alkynol of formula (II) with an amine selected from ammonia, primary or secondary amines or salts thereof to give an alkynamine of formula (III): formula (III) c) reducing the alkynamine of formula (III) to give an allylic amine of formula (IV): formula (IV). Processes to chiral allylic amines of formula (IVa) and (IVb) are also provided.
摘要翻译：提供了制备式（IV）的式（IV）的方法：式（IV），其包括：a）使式（I）的炔醇：式（I）与活化剂反应，得到式（I）的活化炔醇 II）：式（II）OR 3是离去基团，b）使式（II）的活化炔醇与选自氨，伯或仲胺或其盐的胺反应，得到式（III）的炔胺，式（III）c）还原式（III）的炔胺，得到式（IV）的烯丙基胺：式（IV）。还提供了式（IVa）和（IVb）的手性烯丙基胺的方法。

3. 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

4. 发明申请

WO2006046056A1 PROCESS FOR THE TRANSFER HYDROGENATION OF AN ORGANIC COMPOUND IN THE PRESENCE OF A CATALYST REGENERATOR 审中-公开
标题翻译：有机化合物在催化剂再生器存在下的转移加氢方法
公开(公告)号：WO2006046056A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004171
申请日：2005-10-27
申请人： AVECIA PHARMACEUTICALS LIMITED , HODGES, George, Robert , STIRLING, Matthew, John
发明人： HODGES, George, Robert , STIRLING, Matthew, John
IPC分类号： C07B31/00 , C07C29/145
CPC分类号： C07C29/143 , C07B31/00 , Y02P20/584 , C07C33/22 , C07C33/46
摘要： There is provided a process for the transfer hydrogenation of an organic compound having a carbon-carbon or carbon-heteroatom double bond wherein an organic compound of formula (I): wherein: X represents CR 3 R 4 , NR 5 , (NR 5 R 6 ) + Q - , O or S; Q - represents an anion; R 1 , R 2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl or an optionally substituted heterocyclyl group; R 3 , R 4 , and R 6 each independently represents a hydrogen atom, an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl or an optionally substituted heterocyclyl group; R 5 independently represents a hydrogen atom, an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group or a removable group; or one or more of R 1 & R 2 , R 1 & R 3 , R 2 & R 4 , R 3 & R 4 , R 1 & R 5 , R 2 & R 6 and R 5 & R 6 optionally being linked in such a way as to form an optionally substituted ring(s), is reacted with a hydrogen donor in the presence of a transfer hydrogenation catalyst, and substantially in the presence of a catalyst regenerator. Catalyst regenerators include oxidants, for example KMnO 4 , oxygen and oxygen/inert gas mixtures.
摘要翻译：提供了具有碳 - 碳或碳 - 杂原子双键的有机化合物的转移氢化方法，其中式（I）的有机化合物：其中：X表示CR 3 R SUP > 4 ，NR 5，（NR 5 R 6）6 - ，O或S; Q 表示阴离子; R 1，R 2各自独立地表示任选取代的烃基，全卤代烃基或任选取代的杂环基; R 3，R 4和R 6各自独立地表示氢原子，任选取代的烃基，全卤代烃基或任选取代的杂环基组; R 5独立地表示氢原子，任选取代的烃基，全卤代烃基，任选取代的杂环基或可除去的基团; 或R 1，R 2，R 2，R 3和R 3中的一个或多个， R＆lt; 3＆gt;＆lt; 4＆gt;，＆lt; 1＆gt;＆lt; 5＆gt; 任选地在这样的一个或多个连接在一起的第二个和第六个和第六个和第六个和第六个在形成任选取代的环的方式与氢供体在转移氢化催化剂的存在下，基本上在催化剂再生器的存在下反应。催化剂再生器包括氧化剂，例如KMnO 4，氧和氧/惰性气体混合物。

5. 发明申请

WO2006046059A1 CATALYST COMPOSITIONS AND THEIR USE IN THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES 审中-公开
标题翻译：催化剂组合物及其在完全充分增强底物中的应用
公开(公告)号：WO2006046059A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004176
申请日：2005-10-27
申请人： AVECIA PHARMACEUTICALS LIMITED , BLACKER, Andrew, John , STIRLING, Matthew, John
发明人： BLACKER, Andrew, John , STIRLING, Matthew, John
IPC分类号： C07B55/00
CPC分类号： C07B55/00
摘要： There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group V heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred catalyst systems include transition metal halide complex of the formula M n X p Y r wherein M is a transition metal; X is a halide; Y is a neutral optionally substituted hydrocarbyl complexing group, a neutral optionally substituted perhalogenated hydrocarbyl complexing group, or an optionally substituted cyclopentadienyl complexing group; and n, p and r are integers. The reaction promoter is preferably a halide salt.
摘要翻译：提供了对富含对映体的组合物进行去富集的方法，该方法包括使包含至少第一对映异构体或包含碳 - 杂原子键的底物的非对映异构体的对映异构体富集的组合物反应，其中碳是手性中心，杂原子是 V族杂原子，在催化剂体系和任选的反应促进剂的存在下，得到包含具有碳 - 杂原子键的基材的第一和第二对映异构体或非对映异构体的产物组合物，第二对映异构体或二聚异构体的比例在产物组成大于对映异构体富集组合物中第二至第一对映异构体或二聚异构体的比例。优选的催化剂体系包括式M的过渡金属卤化物络合物，其中M是过渡金属; X是卤化物; Y是中性任选取代的烃基络合基团，中性任选取代的全卤代烃基络合基团或任选取代的环戊二烯基络合基团; 并且n，p和r是整数。反应促进剂优选为卤化物盐。

6. 发明申请

WO2005123932A2 PROCESS FOR THE PREPARATION OF ALPHA-SUBSTITUTED CARBOXYLIC ACIDS OR ALPHA-SUBSTITUTED CARBOXYLIC ACID AMIDES 审中-公开
标题翻译：制备ALPHA取代的羧酸或ALPHA取代的羧酸酰胺的方法
公开(公告)号：WO2005123932A2
公开(公告)日：2005-12-29
申请号：PCT/GB2005/002302
申请日：2005-06-10
申请人： AVECIA PHARMACEUTICALS LIMITED , HAZELL, Keith , HOLT, Robert, Antony , RIGBY, Stuart, Richard
发明人： HAZELL, Keith , HOLT, Robert, Antony , RIGBY, Stuart, Richard
IPC分类号： C12P7/40
CPC分类号： C12P7/40 , C12P11/00 , C12P13/02 , C12P13/04 , C12P41/00
摘要： There is provided a process for the preparation of an optically active carboxylic acid or an optically active carboxylic acid amide wherein a carboxylic acid amide having an alpha-carbon substituted with a heteroatom group is enantioselectively hydrolysed in the presence of an enzyme obtainable from Pseudomonas fluorescens to give an optically active carboxylic acid or an optically active carboxylic acid amide. The carboxylic acid amide is preferably a carboxylic acid amide of formula (1): wherein R 1 and R 2 each independently are hydrogen or a substituent group; and R 3 is an optionally substituted heteroatom group; provided that R 1 , R2 and R 3 are different, and the carboxylic acid is preferably a carboxylic acid of formula (4): wherein R 1 and R 2 each independently are hydrogen or a substituent group; and R 3 is an optionally substituted heteroatom group; provided that R 1 , R 2 and R 3 are different such that * is a chiral centre.
摘要翻译：提供了一种制备光学活性羧酸或光学活性羧酸酰胺的方法，其中具有被杂原子基团取代的α-碳的羧酸酰胺在可从荧光假单胞菌获得的酶存在下被对映选择性地水解，得到光学活性羧酸或光学活性羧酸酰胺。羧酸酰胺优选为式（1）的羧酸酰胺：其中R 1和R 2各自独立地为氢或取代基; 并且R 3是任选取代的杂原子基团; 条件是R 1，R 2和R 3不同，并且羧酸优选为式（4）的羧酸：其中R 1和R 2各自独立地为氢或取代基; 并且R 3是任选取代的杂原子基团; 条件是R 1，R 2和R 3不同，使得*是手性中心。

7. 发明申请

WO2005080265A3 PROCESS FOR PREPARING LITHIUM AMIDE AND A COMPOSITION OBTAINABLE BY SAID PROCESS 审中-公开
公开(公告)号：WO2005080265A3
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000480
申请日：2005-02-14
申请人： AVECIA PHARMACEUTICALS LIMITED , ARCHER, Ian, Victor, James , HAMILL, Noel, Anthony
发明人： ARCHER, Ian, Victor, James , HAMILL, Noel, Anthony
IPC分类号： C01B21/092
摘要： There is provided a process for preparing a lithium amide composition in which in a first step lithium metal is brought into contact with ammonia to form lithium bronze and in a second step the lithium bronze is reacted with a 1,3-diene or an arylolefin, such as butadiene, isoprene, piperylene, dimethylbutadiene, hexadiene, styrene, methyl styrene, divinylbenzene, naphthalene or anthracene, in the presence of a solvent wherein the temperature is maintained at or below the boiling point of ammonia. Examples of solvents include pentane, cyclopentane, hexane, heptane, octane, cyclohexane, toluene, xylene, cumene, ethyl benzene, tetraline, diethyl ether, tetrahydrofuran (THF), 2-methyl-THF, tetrahydropyran, diisopropyl ether, dibutyl ether, dioxan, methyl-tert-butyl ether or glycol ether. Lithium amide compositions obtainable by said process show improved activity, particularly in reactions involving enolate formation.

8. 发明申请

WO2005058804A1 PROCESS FOR THE PREPARATION OF TERTIARY AMINES ATTACHED TO A SECONDARY CARBON CENTRE 审中-公开
标题翻译：制备连接到二级碳中心的仲胺的方法
公开(公告)号：WO2005058804A1
公开(公告)日：2005-06-30
申请号：PCT/GB2004/005199
申请日：2004-12-08
申请人： AVECIA PHARMACEUTICALS LIMITED , FIELDHOUSE, Robin
发明人： FIELDHOUSE, Robin
IPC分类号： C07C269/06
CPC分类号： C07C29/143 , C07B2200/07 , C07C269/06 , C07C271/42 , C07C33/20 , C07C33/24
摘要： There is provided a process for the preparation of a compound of Formula: (1) wherein Ar represents an optionally substituted hydrocarbyl or an optionally substituted heterocyclyl group comprising an aromatic moiety; and R 1 , R 2 and R 3 each independently represent an optionally substituted hydrocarbyl or an optionally substituted heterocyclyl group; said process comprising: a) reducing a compound of Formula: (2) to form a compound of Formula: (3) b) activating the compound of Formula: (3) to form a compound of Formula: (4) wherein X represents a leaving group; and c) coupling the compound of Formula: (4) to a compound of Formula: (5) to form a compound of Formula: (1). Stereoselective processes are also provided.
摘要翻译：提供了制备式（1）化合物的方法，其中Ar表示任选取代的烃基或任选取代的包含芳族部分的杂环基; 且R 1，R 2和R 3各自独立地表示任选取代的烃基或任选取代的杂环基; 所述方法包括：a）还原式（2）的化合物以形成式（3）的化合物：b）活化式（3）的化合物以形成式（4）的化合物，其中X表示离开组和c）将式（4）的化合物与式（5）的化合物偶联以形成式（1）的化合物。还提供了立体选择性方法。

9. 发明申请

WO2006067395A1 PROCESS 审中-公开
标题翻译：处理
公开(公告)号：WO2006067395A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004882
申请日：2005-12-14
申请人： AVECIA PHARMACEUTICALS LIMITED , HODGES, George, Robert , MARTIN, Juliette , HAMMIL, Noel, Anthony , HOUSON, Ian, Nicholas
发明人： HODGES, George, Robert , MARTIN, Juliette , HAMMIL, Noel, Anthony , HOUSON, Ian, Nicholas
IPC分类号： C07C209/16 , C07C211/29 , C07C29/143 , C07C33/20
CPC分类号： C07C211/29 , C07C29/143 , C07C209/16 , C07C33/46
摘要： A process for the preparation of a compound of Formula (1) wherein Ar represents an optionally substituted hydrocarbyl or an optionally substituted heterocyclyl group comprising an aromatic moiety; and R 1 and R 2 each independently represent an optionally substituted hydrocarbyl or an optionally substituted heterocyclyl group; said process comprising: a) reducing a compound of Formula (2) to form a compound of Formula (3): b) activating the compound of Formula (3) to form a compound of Formula (4): wherein OX represents a leaving group; and c) coupling the compound of Formula (4) to a compound of Formula (5): to form a compound of Formula (1). A stereoselective reduction of ketones to alcohols is also disclosed.
摘要翻译：制备式（1）化合物的方法，其中Ar表示任选取代的烃基或任选取代的包含芳族部分的杂环基; R 1和R 2各自独立地表示任选取代的烃基或任选取代的杂环基; 所述方法包括：a）还原式（2）的化合物以形成式（3）的化合物：b）活化式（3）的化合物以形成式（4）的化合物：其中OX表示离去基团 ; 和c）将式（4）的化合物与式（5）的化合物偶合：形成式（1）的化合物。还公开了酮对醇的立体选择性还原。

10. 发明申请

WO2006046062A1 PROCESS FOR THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES 审中-公开
标题翻译：去除强化基底的方法
公开(公告)号：WO2006046062A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004179
申请日：2005-10-27
申请人： AVECIA PHARMACEUTICALS LIMITED , BLACKER, Andrew, John , STIRLING, Matthew, John
发明人： BLACKER, Andrew, John , STIRLING, Matthew, John
IPC分类号： C07B55/00 , C07B31/00 , C07C29/145
CPC分类号： C07B55/00 , C07B2200/07 , C07C29/00 , C07C33/22
摘要： There is provided a process for the de-enrichment of enantiomerically enriched compositions which comprises reacting an enantiomerically enriched composition comprising at least a first enantiomer or diastereomer of a substrate comprising a carbon-heteroatom bond, wherein the carbon is a chiral centre and the heteroatom is a group VI heteroatom, in the presence of a catalyst system and optionally a reaction promoter to give a product composition comprising first and second enantiomers or diastereomers of the substrate having a carbon-heteroatom bond, the ratio of second to first enantiomer or disatereomer in the product composition being greater than the ratio of second to first enantiomer or disatereomer in the enantiomerically enriched composition. Preferred substrates include compounds of Formula (1) wherein: X represents O, S; R 1 , R 2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R 1 & R 2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R 1 and R 2 are selected such that * is a chiral centre. In a preferred process a compound of Formula : (2) wherein: X represents O, S; R 1 , R 2 each independently represents an optionally substituted hydrocarbyl, a perhalogenated hydrocarbyl, an optionally substituted heterocyclyl group; or R 1 & R 2 are optionally linked in such a way as to form an optionally substituted ring(s); provided that R1 and R2 are different, may be obtained.
摘要翻译：提供了对富含对映体的组合物进行去富集的方法，该方法包括使包含至少第一对映异构体或包含碳 - 杂原子键的底物的非对映异构体的对映异构体富集的组合物反应，其中碳是手性中心，杂原子是 VI族杂原子，在催化剂体系和任选的反应促进剂的存在下，得到包含具有碳 - 杂原子键的底物的第一和第二对映异构体或非对映异构体的产物组合物，第二对映异构体或二聚异构体的比例产物组成大于对映异构体富集组合物中第二至第一对映异构体或二聚异构体的比例。优选的底物包括式（1）的化合物，其中：X表示O，S; R 1，R 2各自独立地表示任选取代的烃基，全卤代烃基，任选取代的杂环基; 或R 1和R 2任选地以使得形成任选取代的环的方式连接; 条件是选择R 1和R 2以使得*是手性中心。在优选的方法中，式（2）的化合物其中：X表示O，S; R 1，R 2各自独立地表示任选取代的烃基，全卤代烃基，任选取代的杂环基; 或R 1和R 2任选地以使得形成任选取代的环的方式连接; 只要R1和R2不同，就可以得到。

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