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1. 发明申请

WO2010040261A1 PROCESS FOR PREPARING 2-ALKYL-3-AROYL-5-NITRO-BENZOFURANS 审中-公开
标题翻译：制备2-烷基-3-硝基-5-硝基苯并呋喃的方法
公开(公告)号：WO2010040261A1
公开(公告)日：2010-04-15
申请号：PCT/CN2008/072644
申请日：2008-10-10
申请人： LONZA LTD , WELLIG, Alain , RODUIT, Jean-Paul , DAI, Danmei , CHEN, Rongmin
发明人： WELLIG, Alain , RODUIT, Jean-Paul , DAI, Danmei , CHEN, Rongmin
IPC分类号： C07D307/80 , C07C49/76
CPC分类号： C07C45/673 , C07C45/455 , C07C45/71 , C07C251/52 , C07D307/80 , C07C49/84 , C07C49/825
摘要： The present invention relates to a process for the preparation of a compound of formula (I), wherein R 1 is selected from C 1-6 -alkyl, C 3-6 -cycloalkyl and aralkyl, and wherein R 2 at each occurrence independently is halogen or C 1-6 -alkyl, and m is an integer from 0 to 4, Q is selected from halogen, -NO 2 and -NR 3 R 4 , wherein R 3 and R 4 are independently selected from hydrogen, C 1-6 -alkyl, C 3-6 -cycloalkyl, aryl, aralkyl, mesyl and tosyl, or wherein R 3 and R 4 together form a C 4-6 -alkylene group, Y at each occurrence is hydrogen or a hydroxy protection group W that can be hydrolytically cleaved under acidic conditions, and n is an integer from 1 to 3, and n is an integer from 1 to 3, with the proviso that n and m together are not greater than 5.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R 1选自C 1-6 - 烷基，C 3-6 - 环烷基和芳烷基，并且其中R 2在每次出现时独立地为卤素或C1- 并且m是0至4的整数，Q选自卤素，-NO 2和-NR 3 R 4，其中R 3和R 4独立地选自氢，C 1-6 - 烷基，C 3-6 - 环烷基，芳基，芳烷基，甲磺酰基和甲苯磺酰基，或其中R3和R4一起形成C4-6亚烷基，Y在每次出现时为氢或可在酸性条件下水解切割的羟基保护基W，n为1〜 3，n为1〜3的整数，条件是n和m不大于5。

2. 发明申请

WO2011029596A1 PROCESS FOR PREPARING 2-AMINOTHIAZOL-4-YL-ACETIC ACID DERIVATES 审中-公开
标题翻译：制备2-氨基四氢-4-戊酸衍生物的方法
公开(公告)号：WO2011029596A1
公开(公告)日：2011-03-17
申请号：PCT/EP2010/005538
申请日：2010-09-09
申请人： LONZA LTD , DAI, Danmei , ZHU, Wei , WANG, Siming
发明人： DAI, Danmei , ZHU, Wei , WANG, Siming
IPC分类号： C07D277/38 , A61K31/426
CPC分类号： C07D277/40
摘要： The invention provides a process for preparing a (2-aminothiazol-4-yl)-triarylmethyloxy- iminoacetic acid of the formula (I) or an ester thereof of the formula (II) wherein R 1 , R 2 and R 3 independently are optionally substituted phenyl groups and R 4 is C 1-6 alkyl, by reacting a (2-aminothiazol-4-yl)hydroxyiminoacetic acid ester of the formula (III) wherein R 4 is as defined above, with an alcohol of the formula R 1 R 2 R 3 COH, wherein R 1 , R 2 and R 3 are as defined above, in the presence of BF 3 to form a (2-aminothiazol-4-yl)triaryl-methyloxyiminoacetic acid ester of the formula (II), and, optionally, hydrolyzing said ester of formula (II) to obtain the acid of formula (I).
摘要翻译：本发明提供了制备式（I）的（2-氨基噻唑-4-基） - 三芳基甲氧基 - 亚氨基乙酸或其式（II）的酯的方法，其中R 1，R 2和R 3独立地是任选取代的苯基和R 4是C 1-6烷基，其中R 4如上定义的式（III）的（2-氨基噻唑-4-基）羟基亚氨基乙酸酯与式R 1 R 2 R 3 COH的醇反应，其中R1，R2和R3 在BF 3存在下形成式（II）的（2-氨基噻唑-4-基）三芳基 - 甲氧基亚氨基乙酸酯，和任选地水解所述式（II）的酯以获得酸的式（I）化合物。

3. 发明申请

WO2012097511A1 DMP-266 BY CYCLISATION 审中-公开
标题翻译： DMP-266循环
公开(公告)号：WO2012097511A1
公开(公告)日：2012-07-26
申请号：PCT/CN2011/070403
申请日：2011-01-19
申请人： LONZA LTD , LONZA GUANGZHOU RESEARCH AND DEVELOPMENT CENTER LTD , DAI, Danmei , LONG, Xiangtian , LUO, Bing , KULESZA, Anna , REICHWAGEN, Jens , GUO, Yanming
发明人： DAI, Danmei , LONG, Xiangtian , LUO, Bing , KULESZA, Anna , REICHWAGEN, Jens , GUO, Yanming
IPC分类号： C07C271/12 , C07D265/18
CPC分类号： C07D471/08 , C07C29/42 , C07C45/455 , C07C213/00 , C07C269/02 , C07C303/38 , C07C2601/02 , C07D265/18 , C07C271/12 , C07C215/32 , C07C311/17 , C07C49/80 , C07C33/50
摘要： Disclosed is a method for the preparation of the HIV drug Efavirenz, also known as DMP-266, starting from 1,4-dichlorobenzene, and its intermediates.
摘要翻译：公开了一种从1,4-二氯苯及其中间体制备HIV药物依法韦伦（也称为DMP-266）的方法。

4. 发明申请

WO2012097510A1 PROCESS FOR PREPARATION OF EFAVIRENZ BY CYCLISATION 审中-公开
标题翻译：通过循环制备艾维菌素的方法
公开(公告)号：WO2012097510A1
公开(公告)日：2012-07-26
申请号：PCT/CN2011/070396
申请日：2011-01-19
申请人： LONZA LTD , LONZA GUANGZHOU RESEARCH AND DEVELOPMENT CENTER LTD , DAI, Danmei , LONG, Xiangtian , LUO, Bing , KULESZA, Anna , REICHWAGEN, Jens , GUO, Yanming
发明人： DAI, Danmei , LONG, Xiangtian , LUO, Bing , KULESZA, Anna , REICHWAGEN, Jens , GUO, Yanming
IPC分类号： C07D265/18 , C07D269/02
CPC分类号： C07D265/18
摘要： The invention disclosed a process for the preparation of the HIV drug Efavirenz, also known as DMP-266, starting from 1,4-dichlorobenzene, and its intermediates.
摘要翻译：本发明公开了从1,4-二氯苯及其中间体制备HIV药物依法韦伦（也称为DMP-266）的方法。

5. 发明申请

WO2012112922A1 METHODS FOR SYNTHESIZING MOLYBDOPTERIN PRECURSOR Z DERIVATIVES 审中-公开
标题翻译：合成MOLYBDOPTERIN前体Z衍生物的方法
公开(公告)号：WO2012112922A1
公开(公告)日：2012-08-23
申请号：PCT/US2012/025689
申请日：2012-02-17
申请人： ALEXION PHARMACEUTICALS, INC. , LONG, Xiangtian , DAI, Danmei , BRUNNER, Andreas , WATT, Derek Kevin , CLINCH, Keith , BAARS, Sylvia Myrna , DIXON, Rachel Anne , LITTLE, Gillian Mary , LANDREAU, Cyrille Abel Sébastien , PROISY, Nicolas Georges Rene
发明人： LONG, Xiangtian , DAI, Danmei , BRUNNER, Andreas , WATT, Derek Kevin , CLINCH, Keith , BAARS, Sylvia Myrna , DIXON, Rachel Anne , LITTLE, Gillian Mary , LANDREAU, Cyrille Abel Sébastien , PROISY, Nicolas Georges Rene
IPC分类号： A01N57/00 , A61K31/665
CPC分类号： C07F9/65744 , C07D491/14 , C07D491/147
摘要： Provided herein are synthetic methods for preparing a compound of formula (I): Also provided herein are synthetic methods for preparing a compound of formula (XIII): The disclosure also provides useful intermediates, derivatives, prodrugs, and pharmaceutically acceptable salts, solvates and hydrates of the formula (I) and formula (XIII) compounds. These compounds are useful for treating diseases associated with molybdenum cofactor deficiency.
摘要翻译：本文提供了制备式（I）化合物的合成方法：本文还提供了制备式（XIII）化合物的合成方法：本公开还提供了有用的中间体，衍生物，前药和药学上可接受的盐，溶剂合物和水合物的式（I）和式（XIII）化合物。这些化合物可用于治疗与钼辅因子缺乏相关的疾病。

6. 发明公开

EP2344467A1 PROCESS FOR PREPARING 2-ALKYL-3-AROYL-5-NITRO-BENZOFURANS 审中-公开
标题翻译：制备2-烷基-3-芳酰基-5-硝基苯并呋喃的方法
公开(公告)号：EP2344467A1
公开(公告)日：2011-07-20
申请号：EP08877230.6
申请日：2008-10-10
申请人： Lonza Ltd.
发明人： WELLIG, Alain , RODUIT, Jean-Paul , DAI, Danmei , CHEN, Rongmin
IPC分类号： C07D307/80 , C07C49/76
CPC分类号： C07C45/673 , C07C45/455 , C07C45/71 , C07C251/52 , C07D307/80 , C07C49/84 , C07C49/825
摘要： The present invention relates to a process for the preparation of a compound of formula (I), wherein R
1 is selected from C
1-6 -alkyl, C
3-6 -cycloalkyl and aralkyl, and wherein R
2 at each occurrence independently is halogen or C
1-6 -alkyl, and m is an integer from 0 to 4, Q is selected from halogen, -NO
2 and -NR
3 R
4 , wherein R
3 and R
4 are independently selected from hydrogen, C
1-6 -alkyl, C
3-6 -cycloalkyl, aryl, aralkyl, mesyl and tosyl, or wherein R
3 and R
4 together form a C
4-6 -alkylene group, Y at each occurrence is hydrogen or a hydroxy protection group W that can be hydrolytically cleaved under acidic conditions, and n is an integer from 1 to 3, and n is an integer from 1 to 3, with the proviso that n and m together are not greater than 5.
摘要翻译：本发明涉及制备式（I）化合物的方法，其中R 1选自C 1-6 - 烷基，C 3-6 - 环烷基和芳烷基，并且其中R 2在每次出现时独立地为卤素或C 1-6 - 烷基，并且m是0至4的整数，Q选自卤素，-NO 2和-NR 3 R 4，其中R 3和R 4独立地选自氢，C 1-6 - 烷基，C 3-6 - 环烷基，芳基，芳烷基，甲磺酰基和甲苯磺酰基，或者其中R 3和R 4一起形成C 4-6 - 亚烷基，Y在每次出现时为氢或羟基保护基W，在酸性条件下被水解裂解，并且n是1至3的整数，且n是1至3的整数，条件是n和m一起不大于5。

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