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1. 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.

2. 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

3. 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。

4. 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。

5. 发明申请

WO2008012108A3 PROCESS FOR THE PREPARATION OF POLYHYDROXYLATED STILBENES VIA CLAISEN CONDENSATION 审中-公开
公开(公告)号：WO2008012108A3
公开(公告)日：2008-01-31
申请号：PCT/EP2007/006726
申请日：2007-07-30
申请人： PORTELA & CA., S.A. , WIFFEN, Jonathan, William , McCAGUE, Raymond
发明人： WIFFEN, Jonathan, William , McCAGUE, Raymond
IPC分类号： C07C37/50 , C07C67/343 , C07C69/738 , C07C49/84 , C07C43/23 , C07C39/19
摘要： The invention relates to a process for the preparation of polyhydroxylated stilbenes starting from a compound of the formula (I) formula (VI) or formula (IX).

6. 发明申请

WO2003097653A1 COMPOUND AND PROCESSES FOR THE PREPARATION AND USE THEREOF 审中-公开
标题翻译：其制备和使用的化合物和方法
公开(公告)号：WO2003097653A1
公开(公告)日：2003-11-27
申请号：PCT/GB2003/002172
申请日：2003-05-20
申请人： AVECIA LIMITED , WIFFEN, Jonathan, William
发明人： WIFFEN, Jonathan, William
IPC分类号： C07F9/06
CPC分类号： C07F9/6552 , Y02P20/55
摘要： A compound of Formula (1) is provided wherein X represents an optionally substituted hydrocarbyl linking group; R' represents an optionally substituted hydrocarbyl group, P 1 and P 2 are protecting groups, Q represents a group of formula Y, -OZ, or -SZ; Y represents a group forming a Wittig reagent, a P, As or Sb-containing Horner-Wadsworth Emmons or Warren reagent, a P(III), As (III) or Sb(III) precursor of a Horner-Wadsworth Emmons or Warren reagent or an ylid precursor, and Z represents a group forming a P(III), As (III) or Sb(III) precursor of a Horner-Wadsworth Emmons or Warren reagent, or a P(V), As(V) or Sb(V) leaving group.
摘要翻译：提供式（1）的化合物，其中X表示任选取代的烃基连接基团; R'表示任选取代的烃基，P 1和P 2是保护基，Q表示式Y，-OZ或-SZ的基团; Y代表形成Wittig试剂，P，As或Sb的Horner-Wadsworth Emmons或Warren试剂，Horner-Wadsworth Emmons或Warren试剂的P（III），As（III）或Sb（III）或一种内酯前体，Z表示形成Horner-Wadsworth Emmons或Warren试剂的P（III），As（III）或Sb（III）前体或P（V），As（V）或Sb （V）离开组。

7. 发明公开

EP1648866A1 PROCESS AND INTERMEDIATE COMPOUNDS USEFUL IN THE PREPARATION OF STATINS, PARTICULARLY ATORVASTATIN 审中-公开
标题翻译：过程和他汀类药物，生产中间产品特别是阿托伐他汀，适合
公开(公告)号：EP1648866A1
公开(公告)日：2006-04-26
申请号：EP04767938.6
申请日：2004-07-23
申请人： Avecia Pharmaceuticals Limited
发明人： MOODY, David, John , WIFFEN, Jonathan, William
IPC分类号： C07D207/34 , C07D309/10 , C07D309/30 , C07D405/06
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 R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 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; P1 represents hydrogen or a protecting group, and W represents =0 or -OP2, in which P2 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 -OP2, 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.

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