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1. 发明授权

US08865899B2 Chemical process for the synthesis of 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline 有权
标题翻译：用于合成4-（4-溴-2-氟苯胺基）-6-甲氧基-7-（1-甲基哌啶-4-基甲氧基）喹唑啉的化学方法
公开(公告)号：US08865899B2
公开(公告)日：2014-10-21
申请号：US13314034
申请日：2011-12-07
申请人： Jorgen Blixt , Michael David Golden , Philip John Hogan , David Michael Glanville Martin , Francis Joseph Montgomery , Zakariya Patel , John David Pittam , George Joseph Sependa , Christopher John Squire , Nicholas Cartwright Alexander Wright
发明人： Jorgen Blixt , Michael David Golden , Philip John Hogan , David Michael Glanville Martin , Francis Joseph Montgomery , Zakariya Patel , John David Pittam , George Joseph Sependa , Christopher John Squire , Nicholas Cartwright Alexander Wright
IPC分类号： C07D401/12 , C07D239/94 , C07D211/16
CPC分类号： C07D401/12 , C07D211/16 , C07D239/94
摘要： The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline (ZD6474)
摘要翻译：本发明涉及制造某些喹唑啉衍生物的化学方法或其药学上可接受的盐。本发明还涉及制造用于制备喹唑啉衍生物的某些中间体的方法和利用所述中间体制备喹唑啉衍生物的方法。特别地，本发明涉及可用于制备化合物4-（4-溴-2-氟苯胺基）-6-甲氧基-7-（1-甲基哌啶-4-基甲氧基）喹唑啉（ZD6474）的化学方法和中间体，

2. 发明授权

US08163926B2 Process for the synthesis of piperidinyl sulphonate esters 有权
标题翻译：合成哌啶基磺酸酯的方法
公开(公告)号：US08163926B2
公开(公告)日：2012-04-24
申请号：US12088680
申请日：2006-09-27
申请人： Jorgen Blixt , Michael David Golden , Philip John Hogan , David Michael Glanville Martin , Francis Joseph Montgomery , Zakariya Patel , John David Pittam , George Joseph Sependa , Christopher John Squire , Nicholas Cartwright Alexander Wright
发明人： Jorgen Blixt , Michael David Golden , Philip John Hogan , David Michael Glanville Martin , Francis Joseph Montgomery , Zakariya Patel , John David Pittam , George Joseph Sependa , Christopher John Squire , Nicholas Cartwright Alexander Wright
IPC分类号： C07D211/30
CPC分类号： C07D401/12 , C07D211/16 , C07D239/94
摘要： The present invention relates to a process for the manufacture of a compound of the Formula IIa: wherein R is a suitable sulphonate ester; from a (C1-C6)alkyl-4-piperidinecarboxylate compound of the Formula III:
摘要翻译：本发明涉及制备式IIa化合物的方法：其中R是合适的磺酸酯; 由式III的（C 1 -C 6）烷基-4-哌啶羧酸酯化合物：

3. 发明授权

US06531605B1 Process for the manufacture of arylsulfonyl chloride 失效
标题翻译：制备芳基磺酰氯的方法
公开(公告)号：US06531605B1
公开(公告)日：2003-03-11
申请号：US09380478
申请日：1999-10-25
申请人： Philip John Hogan
发明人： Philip John Hogan
IPC分类号： C07B4504
CPC分类号： C07D401/12 , C07C303/02 , Y02P20/55 , C07C309/86 , C07C309/89
摘要： A process is described for the manufacture of a pyridinesulfonyl chloride or a benzenesulfonyl chloride in which the benzene ring bears one or more electron-withdrawing groups, the process comprising reacting a diazonium salt of an aminopyridine or aminobenzene in which the benzene ring bears one or more electron withdrawing groups with a mixture of thionyl chloride in water, in the presence of an electron transfer catalyst.
摘要翻译：描述了制备吡啶磺酰氯或苯磺酰氯的方法，其中苯环带有一个或多个吸电子基团，该方法包括使氨基吡啶或氨基苯的重氮盐与其中苯环带有一个或多个吸电子基团与亚硫酰氯在水中的混合物，在电子转移催化剂的存在下。

4. 发明授权

US4102915A Dimerization process 失效
标题翻译：二进制过程
公开(公告)号：US4102915A
公开(公告)日：1978-07-25
申请号：US793272
申请日：1977-05-03
申请人： James Robert Jennings , Philip John Hogan
发明人： James Robert Jennings , Philip John Hogan
IPC分类号： C07B61/00 , B01J31/00 , B01J31/02 , C07B20060101 , C07C20060101 , C07C67/00 , C07C253/00 , C07C255/09 , C07C120/00 , C07C121/30
CPC分类号： C07C255/00
摘要： Process for the dimerization of ACN to substantially linear C.sub.6 dimers using organic phosphinites or phosphonites as catalyst, in the presence of a proton-donating solvent and optionally a hydrocarbon co-solvent, the ACN and solvent(s) being dry and at least one of the solvents having a boiling point higher than ACN and being capable of rapid phase separation with respect to the dimeric products. Enables the unreacted ACN to be removed by distillation and the solvent(s) and product to be readily separated. Preferably the catalyst partitions in favor of the solvent phase.
摘要翻译：使用有机亚磷酸盐或亚膦酸盐作为催化剂，在质子供体溶剂和任选的烃共溶剂的存在下，将ACN二聚成基本上线性的C6二聚体的方法是ACN和溶剂是干燥的，并且至少一种所述溶剂的沸点高于ACN并且能够相对于二聚产物快速相分离。使未反应的ACN通过蒸馏除去，溶剂和产物容易分离。优选地，催化剂分隔有利于溶剂相。

5. 发明申请

US20120095229A1 CHEMICAL PROCESS 有权
标题翻译：化学工艺
公开(公告)号：US20120095229A1
公开(公告)日：2012-04-19
申请号：US13314034
申请日：2011-12-07
申请人： Jorgen BLIXT , Michael David GOLDEN , Philip John HOGAN , David Michael Glanville MARTIN , Francis Joseph MONTGOMERY , Zakariya PATEL , John David PITTAM , George Joseph SEPENDA , Christopher John SQUIRE , Nicholas Cartwright Alexander WRIGHT
发明人： Jorgen BLIXT , Michael David GOLDEN , Philip John HOGAN , David Michael Glanville MARTIN , Francis Joseph MONTGOMERY , Zakariya PATEL , John David PITTAM , George Joseph SEPENDA , Christopher John SQUIRE , Nicholas Cartwright Alexander WRIGHT
IPC分类号： C07D401/12 , C07D239/94
CPC分类号： C07D401/12 , C07D211/16 , C07D239/94
摘要： The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.
摘要翻译：本发明涉及制造某些喹唑啉衍生物的化学方法或其药学上可接受的盐。本发明还涉及制造用于制备喹唑啉衍生物的某些中间体的方法和利用所述中间体制备喹唑啉衍生物的方法。特别地，本发明涉及可用于制备4-（4-溴-2-氟苯胺基）-6-甲氧基-7-（1-甲基哌啶-4-基甲氧基）喹唑啉化合物的化学方法和中间体。

6. 发明申请

US20080161565A1 Chemical Process 失效
标题翻译：化学工艺
公开(公告)号：US20080161565A1
公开(公告)日：2008-07-03
申请号：US10598116
申请日：2005-02-17
申请人： Margaret Anne Butlin , Roger John Butlin , Philip John Hogan , Andreas Meudt
发明人： Margaret Anne Butlin , Roger John Butlin , Philip John Hogan , Andreas Meudt
IPC分类号： C07D231/10 , C07F9/06 , C07D241/10
CPC分类号： C07D401/14 , C07D413/14 , C07F5/025 , Y02P20/55
摘要： Process for preparing compounds of Formula (I); and (IV); are described.
摘要翻译：制备式（I）化合物的方法; 和（IV）; 被描述。

7. 发明申请

US20090203905A1 CHEMICAL PROCESS 有权
标题翻译：化学工艺
公开(公告)号：US20090203905A1
公开(公告)日：2009-08-13
申请号：US12088680
申请日：2006-09-27
申请人： Jorgen Blixt , Michael David Golden , Philip John Hogan , David Michael Glanville Martin , Francis Joeph Montgomery , Zakariya Patel , John David Pittam , George Joseph Sependa , Christopher John Squire , Nicholas Cartwright Alexander Wright
发明人： Jorgen Blixt , Michael David Golden , Philip John Hogan , David Michael Glanville Martin , Francis Joeph Montgomery , Zakariya Patel , John David Pittam , George Joseph Sependa , Christopher John Squire , Nicholas Cartwright Alexander Wright
IPC分类号： C07D401/12 , C07D211/30 , C07D239/94
CPC分类号： C07D401/12 , C07D211/16 , C07D239/94
摘要： The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline.
摘要翻译：本发明涉及制造某些喹唑啉衍生物的化学方法或其药学上可接受的盐。本发明还涉及制造用于制备喹唑啉衍生物的某些中间体的方法和利用所述中间体制备喹唑啉衍生物的方法。特别地，本发明涉及可用于制备4-（4-溴-2-氟苯胺基）-6-甲氧基-7-（1-甲基哌啶-4-基甲氧基）喹唑啉化合物的化学方法和中间体。

8. 发明申请

US20100094010A1 CHEMICAL PROCESS 审中-公开
标题翻译：化学工艺
公开(公告)号：US20100094010A1
公开(公告)日：2010-04-15
申请号：US12580704
申请日：2009-10-16
申请人： Margaret Anne Butlin , Roger John Butlin , Philip John Hogan , Andreas Meudt
发明人： Margaret Anne Butlin , Roger John Butlin , Philip John Hogan , Andreas Meudt
IPC分类号： C07D413/14 , C07F5/02
CPC分类号： C07D401/14 , C07D413/14 , C07F5/025 , Y02P20/55
摘要： Processes for preparing compounds of Formula I and IV are described.
摘要翻译：描述了制备式I和IV化合物的方法。

9. 发明授权

US07626020B2 Protected forms of N-(3-methoxy-5-methylpiperazin-2-yl)-2-(4-[1,3,4,-oxadiazol-2-yl]phenyl)-pyridine-3-sulphonamide 失效
标题翻译：保护形式的N-（3-甲氧基-5-甲基哌嗪-2-基）-2-（4- [1,3,4， - 二唑-2-基]苯基） - 吡啶-3-磺酰胺
公开(公告)号：US07626020B2
公开(公告)日：2009-12-01
申请号：US10598116
申请日：2005-02-17
申请人： Margaret Anne Butlin , Roger John Butlin , Philip John Hogan , Andreas Meudt
发明人： Margaret Anne Butlin , Roger John Butlin , Philip John Hogan , Andreas Meudt
IPC分类号： C07F9/02
CPC分类号： C07D401/14 , C07D413/14 , C07F5/025 , Y02P20/55
摘要： The invention relates to compounds such as where P is a nitrogen-protecting group, and to processes for preparing these compounds.
摘要翻译：本发明涉及化合物，例如其中P是氮保护基团，以及制备这些化合物的方法。

10. 发明授权

US06943254B2 Synthesis of pyrazinyl pyridine-3-sulfonamide compounds 失效
标题翻译：吡嗪基吡啶-3-磺酰胺化合物的合成
公开(公告)号：US06943254B2
公开(公告)日：2005-09-13
申请号：US10348229
申请日：2003-01-22
申请人： Philip John Hogan
发明人： Philip John Hogan
IPC分类号： C07D213/71 , C07B45/04 , C07C303/02 , C07C309/86 , C07C309/89 , C07D401/12 , C07D241/22
CPC分类号： C07D401/12 , C07C303/02 , Y02P20/55 , C07C309/86 , C07C309/89
摘要： A process for the manufacture of: wherein R is (1-4C)alkyl, carboxyl(1-4C)alkyl or 1,3,4-oxadiazol-2-yl comprises: (a) reaction of the diazonium salt of 3-amino-2-chloropyridine with thionyl chloride in water and an electron transfer catalyst; (b) reaction with isobutyl-(3-methoxy-5-methylpyrazin-2-yl)carbamate and an alkali metal hydride in inert solvent; and (I) where R is (1-4C)alkyl, carboxy(1-4C)alkyl: (c) reaction with a boronic acid: (or an anhydride or ester therof) in the presence of a base and a palladium or nickel catalyst in solvent; and removal of the isobutoxy carbonyl group; or (ii) where R is 1,3,4-oxadiazol-2-yl (c) reaction with 4-methoxycarbonylphenylboronic acid (or an anhydride or ester thereof) with a source fluoride ion under aqueous conditions; (d) removal of the isobutoxycarbonyl protecting group; (e) conversion of the methyl ester group to the hydrazide; and (f) conversion to a 1,3,4-oxadiazol-2-yl moiety.
摘要翻译：一种制备方法：其中R是（1-4C）烷基，羧基（1-4C）烷基或1,3,4-恶二唑-2-基包括：（a）3-氨基的重氮盐 -2-氯吡啶与亚硫酰氯在水中的电子转移催化剂; （b）与惰性溶剂中的异丁基 - （3-甲氧基-5-甲基吡嗪-2-基）氨基甲酸酯和碱金属氢化物反应; 和（I）其中R是（1-4C）烷基，羧基（1-4C）烷基：（c）在碱和钯或镍的存在下与硼酸（或酸酐或酯基）反应：溶剂中的催化剂; 并除去异丁氧基羰基; 或（ii）其中R是1,3,4-恶二唑-2-基（c）在含水条件下与4-氟甲基羰基苯基硼酸（或其酸酐或酯）与源氟离子反应; （d）除去异丁氧羰基保护基; （e）甲酯转化为酰肼; 和（f）转化为1,3,4-恶二唑-2-基部分。

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