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1. 发明专利

IL182589D0 PROCESS FOR THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES 未知
公开(公告)号：IL182589D0
公开(公告)日：2007-07-24
申请号：IL18258907
申请日：2007-04-16
申请人： AVECIA PHARMACEUTICALS LTD , BLACKER ANDREW JOHN , STIRLING MATTHEW JOHN
IPC分类号： C07B20100101 , C07B55/00 , C07C29/00
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 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.

2. 发明专利

IL182590D0 CATALYST COMPOSITIONS AND THEIR USE IN THE DE-ENRICHMENT OF ENANTIOMERICALLY ENRICHED SUBSTRATES 未知
公开(公告)号：IL182590D0
公开(公告)日：2007-07-24
申请号：IL18259007
申请日：2007-04-16
申请人： AVECIA PHARMACEUTICALS LTD , BLACKER ANDREW JOHN , STIRLING MATTHEW JOHN
IPC分类号： C07B20100101
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 diastereomer in the product composition being greater than the ratio of second to first enantiomer or diastereomer in the enantiomerically enriched composition. Preferred catalyst systems include transition metal halide complex of the formula MnXpYr 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.

3. 发明申请

WO2003004459A2 PROCESS FOR THE PREPARATION OF NITRILE COMPOUNDS 审中-公开
标题翻译：制备腈化合物的方法
公开(公告)号：WO2003004459A2
公开(公告)日：2003-01-16
申请号：PCT/GB2002/002964
申请日：2002-06-27
申请人： AVECIA LIMITED , BLACKER, Andrew, John , HOUSON, Ian, Nicholas , WIFFEN, Jonathan, William
发明人： BLACKER, Andrew, John , HOUSON, Ian, Nicholas , WIFFEN, Jonathan, William
IPC分类号： C07C253/16
CPC分类号： C07D319/06 , C07C253/16 , Y02P20/55 , C07C255/12
摘要： A process is provided for the preparation of a compound of Formula (1) wherein: R 1 is H, optionally substituted acyl, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl: R² and R³ each independently are H or a hydroxy protecting group; comprising the steps: (a) reacting a compound of Formula (2) in a solvent in the presence of a base with a compound of formula R 4 SO 2 X to give a compound of Formula (3); wherein: R 4 is an optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl group; and X is halogen: and (b) reacting the compound of Formula (3) with a cyanide source in the presence of a phase transfer catalyst.
摘要翻译：提供了制备式（1）化合物的方法，其中：R 1为H，任选取代的酰基，任选取代的烷基，任选取代的芳基或任选取代的取代的杂芳基：R' 和R＆sup3; 各自独立地为H或羟基保护基; 包括以下步骤：（a）使式（2）化合物在溶剂中在碱存在下与式R 4 SO 2 X化合物反应，得到式（3）的化合物; 其中：R 4是任选取代的烷基，任选取代的芳基或任选取代的杂芳基; X是卤素;和（b）使式（3）化合物与氰化物源在相转移催化剂存在下反应。

4. 发明申请

WO03004459A3 PROCESS FOR THE PREPARATION OF NITRILE COMPOUNDS 审中-公开
标题翻译：制备NITRILE化合物的方法
公开(公告)号：WO03004459A3
公开(公告)日：2003-05-01
申请号：PCT/GB0202964
申请日：2002-06-27
申请人： AVECIA LTD , BLACKER ANDREW JOHN , HOUSON IAN NICHOLAS , WIFFEN JONATHAN WILLIAM
发明人： BLACKER ANDREW JOHN , HOUSON IAN NICHOLAS , WIFFEN JONATHAN WILLIAM
IPC分类号： C07B61/00 , C07C253/16 , C07C255/12 , C07C255/13 , C07C255/17 , C07C255/20 , C07C255/36 , C07C255/37 , C07C255/40 , C07D319/06
CPC分类号： C07D319/06 , C07C253/16 , Y02P20/55 , C07C255/12
摘要： A process is provided for the preparation of a compound of Formula (1) wherein: R is H, optionally substituted acyl, optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl: R² and R³ each independently are H or a hydroxy protecting group; comprising the steps: (a) reacting a compound of Formula (2) in a solvent in the presence of a base with a compound of formula R SO2X to give a compound of Formula (3); wherein: R is an optionally substituted alkyl, optionally substituted aryl or optionally substituted heteroaryl group; and X is halogen: and (b) reacting the compound of Formula (3) with a cyanide source in the presence of a phase transfer catalyst.
摘要翻译：提供了制备式（1）化合物的方法，其中：R 1是H，任选取代的酰基，任选取代的烷基，任选取代的芳基或任选取代的杂芳基：R 2和R 3各自独立地是H或羟基保护组包括以下步骤：（a）使式（2）的化合物在碱的存在下在溶剂中与式R 4 SO 2 X的化合物反应，得到式（3）的化合物; 其中：R 4是任选取代的烷基，任选取代的芳基或任选取代的杂芳基; 和X是卤素;和（b）在相转移催化剂存在下使式（3）的化合物与氰化物源反应。

5. 发明申请

WO1998028306A1 PROCESS FOR THE PREPARATION OF AN ORGANOZINC REAGENT 审中-公开
标题翻译：制备有机原料试剂的方法
公开(公告)号：WO1998028306A1
公开(公告)日：1998-07-02
申请号：PCT/GB1997003443
申请日：1997-12-15
申请人： ZENECA LIMITED , BLACKER, Andrew, John , FIELDEN, Jan, Michael
发明人： ZENECA LIMITED
IPC分类号： C07F03/06
CPC分类号： C07D213/30 , C07B53/00 , C07B2200/07 , C07C29/40 , C07F3/06 , C07C33/22 , C07C33/46 , C07C33/20
摘要： A process for the preparation of an aromatic organozinc compound is provided. The process comprises reacting a zinc chloride, bromide or iodide and an organometallic compoud of another metal comprising an aromatic moiety, producing a reaction product comprising an organozinc compound and a halide salt of the other metal. The reaction product is then contacted with a liquid hydrocarbon, in which the organozinc compound is soluble and the halide salt of the other metal is of low solubility. The halide salt of the other metal is separated from the hydrocarbon, and the organozinc compound can be recovered from the hydrocarbon. Organozinc compounds produced by this process can be employed to generate chiral centres in suitable substrates.
摘要翻译：提供了一种制备芳香族有机锌化合物的方法。该方法包括使氯化锌，溴化物或碘化物与包含芳族部分的另一种金属的有机金属化合物反应，产生包含有机锌化合物和另一种金属的卤化物盐的反应产物。然后使反应产物与液态烃接触，其中有机锌化合物是可溶的，另一种金属的卤化物盐的溶解度低。另一种金属的卤化物盐与烃分离，有机锌化合物可以从烃中回收。通过该方法制备的有机锌化合物可用于在合适的底物中产生手性中心。

6. 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。

7. 发明申请

WO1996037628A1 PREPARATION OF HYDROXY COMPOUNDS BY BIOCONVERSION WITH DIOXYGENASE 审中-公开
标题翻译：通过二氧化碳生物反应制备羟基化合物
公开(公告)号：WO1996037628A1
公开(公告)日：1996-11-28
申请号：PCT/GB1996001208
申请日：1996-05-20
申请人： ZENECA LIMITED , BLACKER, Andrew, John , BOYD, Derek, Raymond , DALTON, Howard , BOWERS, Nigel
发明人： ZENECA LIMITED
IPC分类号： C12P07/22
CPC分类号： C07C29/48 , C07C247/14 , C07C2602/08 , C07C2602/10 , C07C2602/24 , C12P7/22 , C12P13/00 , C12P13/001 , C12P13/02 , C12P17/00 , C07C35/36 , C07C35/32 , C07C35/48
摘要： A process for preparing a compound of formula (3) in which R is -H; which comprises the steps: (i) conversion of a compound of formula (1) into a compound of formula (2) using a dioxygenase enzyme; (ii) conversion of the compound of formula (2) into a compound of formula (3) wherein is -COR; and (iii) conversion of the compound of formula (3) in which R is -COR into a compound of formula (3) in which R is -H; wherein R , a, b, c, d, Z, m and X are as defined in Claim 1. Also claimed are individual steps of the process and new compounds of formula (2).
摘要翻译：制备其中R 2为-H的式（3）化合物的方法; 其包括以下步骤：（i）使用双加氧酶将式（1）的化合物转化成式（2）的化合物; （ii）将式（2）的化合物转化为式（3）的化合物，其中是-COR; 和（iii）其中R 2为-COR的式（3）化合物转化为其中R 2为-H的式（3）化合物; 其中R 2，a，b，c，d，Z，m和X如权利要求1中所定义。还要求保护的是该方法的单独步骤和式（2）的新化合物。

8. 发明申请

WO1993017994A1 HYDROXY DERIVATIVES OF CYCLOHEXADIENE 审中-公开
标题翻译：环己酮的羟基衍生物
公开(公告)号：WO1993017994A1
公开(公告)日：1993-09-16
申请号：PCT/GB1993000523
申请日：1993-03-12
申请人： ZENECA LIMITED , BLACKER, Andrew, John , BROWN, Stephen, Martin , BOWDEN, Martin, Charles
发明人： ZENECA LIMITED
IPC分类号： C07C67/31
CPC分类号： C12P17/02 , C07C67/31 , C07D307/83 , C12P7/42 , C12P13/00 , C12P13/001 , C12P13/002 , C12P13/008 , C12P13/02 , C07C69/732
摘要： Novel substituted cis-1,2-dihydroxy-cyclohexadiene compounds, useful as intermediates in the production of compounds for use as intermediates in the production of agrochemicals and pharmaceuticals, and a microbial process for the preparation thereof.
摘要翻译：新型取代的顺式-1,2-二羟基 - 环己二烯化合物，可用作制备用于生产农药和药物的中间体的化合物的中间体，以及用于制备其的微生物方法。

9. 发明申请

WO2009037497A1 PROCESS FOR PREPARING SULPHONAMIDES 审中-公开
标题翻译：制备磺酰胺的方法
公开(公告)号：WO2009037497A1
公开(公告)日：2009-03-26
申请号：PCT/GB2008/050769
申请日：2008-09-03
申请人： NPIL PHARMACEUTICALS (UK) LIMITED , BLACKER, Andrew John
发明人： BLACKER, Andrew John
IPC分类号： C07C303/40 , C07C311/18 , C07C311/19
CPC分类号： C07C269/06 , C07C303/38 , Y02P20/55 , C07C271/20 , C07C271/22 , C07C271/52 , C07C271/54
摘要： The present invention relates to a process for preparing a class of sulphonamides which are aspartyl protease inhibitors. These compounds find therapeutic use in the treatment of the human immunodeficiency virus (HIV). This virus is the causative agent for acquired immunodeficiency syndrome (AIDS). The synthetic procedure of the present invention involves a convenient and efficient process utilising base coupling, decarboxylation and reduction steps to produce the desired compounds in good yield. One advantage of the process of the present invention is its convergent approach which leads to improved yields. The procedure also enables stereoselectivity to be controlled to a high degree, thus avoiding the need for resolution procedures where chiral products are formed.
摘要翻译：本发明涉及制备一类为天冬氨酰蛋白酶抑制剂的磺酰胺类的方法。这些化合物可用于治疗人类免疫缺陷病毒（HIV）。这种病毒是获得性免疫缺陷综合征（艾滋病）的病原体。本发明的合成方法包括利用碱偶联，脱羧和还原步骤的方便和有效的方法以高产率生产所需化合物。本发明方法的一个优点是其收敛方法，其导致产量提高。该程序还能够使立体选择性得到高度控制，从而避免手性产物形成时需要解决程序。

10. 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。

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