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1. 发明申请

WO2004076053A3 CHEMICAL PROCESS FOR THE PREPARATION OF INTERMEDIATES TO OBTAIN N-FORMYL HYDROXYLAMINE COMPOUNDS 审中-公开
标题翻译：制备中间体以获得N-甲醛羟基胺化合物的化学方法
公开(公告)号：WO2004076053A3
公开(公告)日：2004-12-02
申请号：PCT/US2004005159
申请日：2004-02-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , PRASHAD MAHAVIR , KIM HANG-YONG , HU BIN , SLADE JOEL , KAPA PRASAD KOTESWARA , GIRGIS MICHAEL JOHN
发明人： PRASHAD MAHAVIR , KIM HANG-YONG , HU BIN , SLADE JOEL , KAPA PRASAD KOTESWARA , GIRGIS MICHAEL JOHN
IPC分类号： A61P31/04 , C07C51/487 , C07C239/20 , C07D401/12 , A61K31/44 , C07B53/00 , C07C259/06
CPC分类号： C07D401/12 , C07B2200/07 , C07C51/487 , C07C239/20 , C07C59/01
摘要： Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo-2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo4-7alkanes or thiazacyclo4-7alkanes, which have one or more of the following features : (1) make use of a particular beta-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxy-propionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products. See Formula (I).
摘要翻译：用于制备可用于制备抗菌N- [1-氧代-2-烷基-3-（N-羟基甲酰氨基） - 丙基} - （羰基氨基 - 芳基或 - 杂芳基） - 偶氮基-4-7烷烃或噻唑烷-4-醇的中间体的改进方法，其具有一个或多个以下特征：（1）利用特定的β-内酰胺中间体; （2），其使用特定的拆分剂，对映体纯的取代的丙酸，特别是（R）-2-丁基-3-羟基 - 丙酸; （3）避免使用过氧化氢; 和（4）促进选择性脱苄基化减少废弃副产物的生产。参见式（I）。

2. 发明申请

WO2004076053A2 CHEMICAL PROCESS 审中-公开
标题翻译：化学工艺
公开(公告)号：WO2004076053A2
公开(公告)日：2004-09-10
申请号：PCT/US2004/005159
申请日：2004-02-20
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , PRASHAD, Mahavir , KIM, Hang-Yong , HU, Bin , SLADE, Joel , KAPA, Prasad, Koteswara , GIRGIS, Michael, John
发明人： PRASHAD, Mahavir , KIM, Hang-Yong , HU, Bin , SLADE, Joel , KAPA, Prasad, Koteswara , GIRGIS, Michael, John
IPC分类号： B01J
CPC分类号： C07D401/12 , C07B2200/07 , C07C51/487 , C07C239/20 , C07C59/01
摘要： Improved processes for preparing intermediates useful for preparing antibacterial N-[1-oxo2-alkyl-3-(N-hydroxyformamido)-propyl}-(carbonylamino-aryl or -heteroaryl)-azacyclo47alkanes or thiazacyclo4-7alkanes, which have one or more of the following features : (1) make use of a particular I3-lactam intermediate; (2) which make use of a particular resolving agents, enantiomerically pure substituted propionic acids, especially (R)-2-butyl-3-hydroxypropionic acid; (3) which avoid the use of hydrogen peroxide; and (4) which facilitate selective debenzylation reducing production of waste by-products.
摘要翻译：制备用于制备抗菌N- [1-氧代-2-烷基-3-（N-羟基甲酰氨基） - 丙基} - （羰基氨基 - 芳基或 - 杂芳基） - 偶氮环戊烷或噻唑烷-4-7烷的中间体的改进方法，其具有一个或多个具有以下特点：（1）利用特定的内酰胺中间体; （2），其使用特定的拆分剂，对映体纯的取代的丙酸，特别是（R）-2-丁基-3-羟基丙酸; （3）避免使用过氧化氢; 和（4）促进选择性脱苄基化减少废弃副产物的生产。

3. 发明申请

WO03008367A3 PROCESS FOR THE MANUFACTURE OF AROMATIC CARBOXYLIC ACIDS FROM ALDEHYDES 审中-公开
标题翻译：从醛类制备芳香羧酸的方法
公开(公告)号：WO03008367A3
公开(公告)日：2003-04-10
申请号：PCT/US0222631
申请日：2002-07-16
申请人： NOVARTIS AG , GIRGIS MICHAEL JOHN , SHEKHAR RATNA
发明人： GIRGIS MICHAEL JOHN , SHEKHAR RATNA
IPC分类号： C07C51/235 , C07C51/255 , C07C63/04 , C07C233/81
CPC分类号： C07C51/235 , C07C63/04
摘要： A low temperature process for preparing an aromatic acid having formula (I), said process comprising reacting an aromatic aldehyde having formula (II) with a gas having an oxygen content of 1 to 100 weight percent, based on the total weight of the gas, at a temperature of about 20 °C to less than 100 °C in the presence of the supported Group VIII metal catalyst, and a solvent having a flash point greater than 95 °C and/or a melting point less than 55 °C, provided that the flash point of the solvent is greater than the reaction temperature, wherein R and R are independently selected from the group consisting of hydrogen and a C1-C8 linear, branched or cyclic alkyl group. The process of the invention yields an aromatic acid in excellent yield, and (i) does not involve the use of deleterious oxidizing agents; (ii) is essentially free of by-products; and (iii) is accomplished at a temperature of less than 100 °C.
摘要翻译：用于制备具有式（I）的芳族酸的低温方法，所述方法包括使具有式（II）的芳族醛与基于气体总重量的1至100重量％的氧含量的气体反应，在负载的第VIII族金属催化剂的存在下，在约20℃至小于100℃的温度和闪点大于95℃和/或熔点小于55℃的溶剂中，提供了溶剂的闪点大于反应温度，其中R 1和R 2独立地选自氢和C 1 -C 8直链，支链或环状的烷基。本发明的方法得到优异的收率的芳香酸，（i）不涉及有害氧化剂的使用; （ii）基本上不含副产物; 和（iii）在小于100℃的温度下完成。

4. 发明申请

WO2003008367A2 PROCESS FOR THE MANUFACTURE OF ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物的制造方法
公开(公告)号：WO2003008367A2
公开(公告)日：2003-01-30
申请号：PCT/US2002/022631
申请日：2002-07-16
申请人： NOVARTIS AG , GIRGIS, Michael, John , SHEKHAR, Ratna
发明人： GIRGIS, Michael, John , SHEKHAR, Ratna
IPC分类号： C07C51/00
CPC分类号： C07C51/235 , C07C63/04
摘要： A low temperature process for preparing an aromatic acid having formula (I), said process comprising reacting an aromatic aldehyde having formula (II) with a gas having an oxygen content of 1 to 100 weight percent, based on the total weight of the gas, at a temperature of about 20 °C to less than 100 °C in the presence of the supported Group VIII metal catalyst, and a solvent having a flash point greater than 95 °C and/or a melting point less than 55 °C, provided that the flash point of the solvent is greater than the reaction temperature, wherein R 1 and R 2 are independently selected from the group consisting of hydrogen and a C 1 -C 8 linear, branched or cyclic alkyl group. The process of the invention yields an aromatic acid in excellent yield, and (i) does not involve the use of deleterious oxidizing agents; (ii) is essentially free of by-products; and (iii) is accomplished at a temperature of less than 100 °C.
摘要翻译：用于制备具有式（I）的芳族酸的低温方法，所述方法包括使具有式（II）的芳族醛与基于气体总重量的1至100重量％的氧含量的气体反应，在负载的VIII族金属催化剂的存在下，在约20℃至小于100℃的温度下，并且提供闪点高于95℃和/或熔点小于55℃的溶剂，提供溶剂的闪点大于反应温度，其中R 1和R 2独立地选自氢和C 1 -C 8直链，支链或环状的烷基。本发明的方法得到优异的收率的芳香酸，（i）不涉及有害氧化剂的使用; （ii）基本上不含副产物; 和（iii）在小于100℃的温度下完成。

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