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1. 发明申请

WO2009056487A1 METHODS FOR STABILIZING LITHIATED HALOGEN-SUBSTITUTED AROMATIC COMPOUNDS 审中-公开
标题翻译：用于稳定取代的取代的芳族化合物的方法
公开(公告)号：WO2009056487A1
公开(公告)日：2009-05-07
申请号：PCT/EP2008/064403
申请日：2008-10-23
申请人： F. HOFFMANN-LA ROCHE AG , JI, Yaohui , RAWALPALLY, Thimma
发明人： JI, Yaohui , RAWALPALLY, Thimma
IPC分类号： C07C45/00 , C07C47/575 , C07C47/55 , C07F1/02
CPC分类号： C07C45/00 , C07C47/55 , C07C47/575
摘要： The present invention provides novel methods for stabilizing lithiated halogen-substituted aromatic compounds. In particular, the method is useful for the preparation of 2-methoxy-5, 6-difluorobenzaldehyde, an important intermediate for the preparation of [4-amino-2-(1-methanesuifonyrpiperidin-4-ylamino) pyrimidin-5-yl](2,3-difluoro- 6methoxyphenyl)methanone, a potent and selective inhibitor of CDK4/Cyclin D1, CDK2/Cyclin E and CDK1/Cyclin B. The method is also useful for stabilizing other lithiated halogen-substituted aromatic compounds and is particularly useful for scale up reactions where the exothermic nature of the reaction can lead to reaction runway. The reaction runaway hazard can be eliminated by using anhydrous MgCl 2 as an additive to complex with and stabilize the reactive species and slow down the rate of decomposition.
摘要翻译：本发明提供了稳定锂化卤素取代的芳族化合物的新方法。特别地，该方法可用于制备2-甲氧基-5,6-二氟苯甲醛，其是制备[4-氨基-2-（1-甲基异烟酰基哌啶-4-基氨基）嘧啶-5-基] （2,3-二氟-6-甲氧基苯基）甲酮，一种有效和选择性的CDK4 /细胞周期蛋白D1，CDK2 /细胞周期蛋白E和CDK1 /细胞周期蛋白B抑制剂。该方法也可用于稳定其他锂化卤素取代的芳族化合物，特别有用用于放大反应，其中反应的放热性质可导致反应跑道。通过使用无水MgCl 2作为与活性物质复合并稳定反应性物质的添加剂可以消除反应失控危险，并降低分解速率。

2. 发明申请

WO2010043515A1 DIAZONIUM-FREE METHOD TO MAKE AN INDAZOLE INTERMEDIATE IN THE SYNTHESIS OF BICYCLIC 5-(TRIFLUORMETHOXY)-1H-3-INDAZOLECARBOXYLIC ACID AMIDES 审中-公开
标题翻译：在双酚5-（三氟甲基）-1H-3-异吲哚酸酰胺的合成中制备吲哚中间体的无氮方法
公开(公告)号：WO2010043515A1
公开(公告)日：2010-04-22
申请号：PCT/EP2009/062952
申请日：2009-10-06
申请人： F. HOFFMANN-LA ROCHE AG , CLEARY, Thomas P. , JI, Yaohui , RAWALPALLY, Thimma
发明人： CLEARY, Thomas P. , JI, Yaohui , RAWALPALLY, Thimma
IPC分类号： C07D231/56 , C07D453/02
CPC分类号： C07D453/02 , C07D231/56
摘要： The present invention provides novel methods for preparing 5-(trifluoromethoxy)-lH-3- indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5- trifluoromethoxy-lH-indazole-S-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
摘要翻译：本发明提供了制备5-（三氟甲氧基）-1H-3-吲哚羧酸（3）的新方法，其是用于制备式（I）的双环-5-三氟甲氧基-1H-吲唑-3-羧酸酰胺的有用前体（1）。式（1）的化合物作为烟碱型α-7受体的激动剂和部分激动剂是活性的，并且正在研究中用于治疗与缺陷或功能异常的烟碱型乙酰胆碱受体（特别是脑）相关的疾病状况，例如治疗阿尔茨海默病和精神分裂症，以及其他精神和神经障碍。本发明的方法可用于按比例制备化合物（3）。

3. 发明申请

WO2008151992A3 A NOVEL PROCESS FOR THE PREPARATION OF 3-AMINO-PENTAN-1,5-DIOL 审中-公开
标题翻译：一种制备3-氨基 - 戊-1-醇的新工艺
公开(公告)号：WO2008151992A3
公开(公告)日：2009-05-28
申请号：PCT/EP2008057072
申请日：2008-06-06
申请人： HOFFMANN LA ROCHE , CLEARY THOMAS P , JI YAOHUI , LEE GARY R , RAWALPALLY THIMMA , SARMA KESHAB
发明人： CLEARY THOMAS P , JI YAOHUI , LEE GARY R , RAWALPALLY THIMMA , SARMA KESHAB
IPC分类号： C07C213/02 , C07C215/10 , C07C269/04 , C07C269/06 , C07C271/16 , C07C271/22
CPC分类号： C07C269/04 , C07C213/08 , C07C213/10 , C07C215/10 , C07C227/08 , C07C227/16 , C07C269/06 , C07C271/16 , C07C271/22 , C07C229/24 , C07C229/30
摘要： The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-l,5-diol (2), which is useful for the preparation of 6-(2,4- difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H- pyrido[2,3-d]pyrimidine-7-one (1) a MAP -kinase inhibitor useful in the treatment of rheumatoid arthritis.
摘要翻译：本发明提供了制备关键中间体3-氨基戊烷-1,5-二醇（2）的新方法，其可用于制备6-（2,4-二氟苯氧基）-2- [3- 羟基-1-（2-羟乙基） - 丙基氨基] -8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮（1）可用于治疗类风湿性关节炎的MAP-激酶抑制剂。

4. 发明申请

WO2008151992A2 A NOVEL PROCESS FOR THE PREPARATION OF 3-AMINO-PENTAN-1,5-DIOL 审中-公开
标题翻译：一种制备3-氨基 - 戊-1-醇的新工艺
公开(公告)号：WO2008151992A2
公开(公告)日：2008-12-18
申请号：PCT/EP2008/057072
申请日：2008-06-06
申请人： F. HOFFMANN-LA ROCHE AG , CLEARY, Thomas, P. , JI, Yaohui , LEE, Gary, R. , RAWALPALLY, Thimma , SARMA, Keshab
发明人： CLEARY, Thomas, P. , JI, Yaohui , LEE, Gary, R. , RAWALPALLY, Thimma , SARMA, Keshab
IPC分类号： C07C213/02 , C07C215/10 , C07C269/04 , C07C269/06 , C07C271/16 , C07C271/22
CPC分类号： C07C269/04 , C07C213/08 , C07C213/10 , C07C215/10 , C07C227/08 , C07C227/16 , C07C269/06 , C07C271/16 , C07C271/22 , C07C229/24 , C07C229/30
摘要： The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-l,5-diol (2), which is useful for the preparation of 6-(2,4- difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H- pyrido[2,3-d]pyrimidine-7-one (1) a MAP -kinase inhibitor useful in the treatment of rheumatoid arthritis.
摘要翻译：本发明提供了制备关键中间体3-氨基戊烷-1,5-二醇（2）的新方法，其可用于制备6-（2,4-二氟苯氧基）-2- [3- 羟基-1-（2-羟乙基） - 丙基氨基] -8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮（1）可用于治疗类风湿性关节炎的MAP-激酶抑制剂。

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