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1. 发明申请

US20100029985A1 Process 审中-公开
标题翻译：处理
公开(公告)号：US20100029985A1
公开(公告)日：2010-02-04
申请号：US11722454
申请日：2005-12-14
申请人： George Robert Hodges , Juliette Martin , Noel Anthony Hammil , Ian Nicholas Houson
发明人： George Robert Hodges , Juliette Martin , Noel Anthony Hammil , Ian Nicholas Houson
IPC分类号： C07C211/27 , C07C37/00
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 R1 and R2 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; 并且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。

2. 发明申请

US20070043221A1 Process and intermediates useful in the preparation of statins, particularly atorvastatin 失效
标题翻译：用于制备他汀类药物，特别是阿托伐他汀的方法和中间体
公开(公告)号：US20070043221A1
公开(公告)日：2007-02-22
申请号：US10563459
申请日：2004-07-23
申请人： David John Moody , Jonathan William Wiffen
发明人： David John Moody , Jonathan William Wiffen
IPC分类号： C07D405/02 , 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 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.
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）使式（1）的化合物氰化：其中Y表示卤素，优选 CI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）化合物：b）还原式（2）化合物得到式（3）化合物：将式（3）化合物与式（4）化合物偶联：得到式（5）化合物：当W表示-OP 2时，将式（5）化合物去保护然后氧化得到式（6）化合物：和e）使化合物当W表示-O时，式（5）或式（6）化合物开环，除去任何残留的保护基，得到式（7）化合物或其盐。

3. 发明申请

US20080281101A1 Process and Intermediate Compounds Useful in the Preparation of Statins, Particularly Rosuvastatin 失效
公开(公告)号：US20080281101A1
公开(公告)日：2008-11-13
申请号：US10594380
申请日：2005-03-23
申请人： David John Moody , Jonathan William Wiffen
发明人： David John Moody , Jonathan William Wiffen
IPC分类号： C07D405/06 , C07D239/42 , C07D309/10 , C07D309/30
CPC分类号： C07D405/06 , C07D309/10 , C07D309/30 , Y02P20/55
摘要： There is provided a process for the preparation of a compound of formula (7): formula (7) wherein R1 represents an alkyl group; R2 represents an aryl group; R3 represents hydrogen, a protecting group or an alkyl group; and R4 represents hydrogen, a protecting group or a SO2R5 group where R5 is an alkyl group, which comprises a) hydroxylating a compound of formula (1): formula (1) wherein Y represents a halo group; P1 represents hydrogen or a protecting group, and W represents ═O or —OP2, in which P2 represents hydrogen or a protecting group, to give a compound of formula (2): formula (2) b) oxidising the compound of formula (2) to give a compound of formula (3): formula (3) c) coupling the compound of formula (3) with a compound of formula (4): formula (4) wherein R3 represents a protecting group or an alkyl group; R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group; and R6 represents (PR7R8)+X− or P(═O)R7R8 in which X is an anion and R7 and R8 each independently is an alkyl, aryl, alkoxy or aryloxy group, to give a compound of formula (5): formula (5) wherein R3 represents a protecting group or an alkyl group; and R4 represents a protecting group or a SO2R5 group where R5 is an alkyl group, d) when W represents —OP2, removing any P2 protecting group and oxidising the compound of formula (5) to give a compound of formula (6): formula (6) and e) subjecting the compound of formula (5) when W represents═O, or compound of formula (6) to ring-opening, removal of any P1 protecting groups, and optionally removing any additional protecting groups to give a compound of formula (7).

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