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公开(公告)号：US20080154063A1
公开(公告)日：2008-06-26
申请号：US12004190
申请日：2007-12-20
IPC分类号： C07C215/10 , C07C213/00 , C07C215/20
CPC分类号： C07C213/02 , C07C215/16 , Y02P20/55 , C07C215/10
摘要： A method of making an amino-alkylenediol and intermediate compounds useful in the method is disclosed. The method includes preparing a first intermediate compound comprising an aminoalkylene diol wherein a protecting group is linked to the amino functionality, and optionally, preparing a second intermediate compound comprising a salt of the first intermediate compound.The first intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, and Z is a protecting group.The second intermediate compound has the structure wherein R is a divalent alkylene radical having from 2 to 20 carbon atoms, X and Y are independently a divalent linking moiety or a single bond, TsO− is toluene sulfonate, and Z is a protecting group.
摘要翻译： 公开了制备用于该方法的氨基亚烷基二醇和中间体化合物的方法。 该方法包括制备包含氨基亚烷基二醇的第一中间体化合物，其中保护基与氨基官能团连接，任选地，制备包含第一中间体化合物的盐的第二中间体化合物。 第一中间体化合物具有其中R为具有2至20个碳原子的二价亚烷基，X和Y独立地为二价连接部分或单键的结构，Z为保护基。 第二中间体化合物具有其中R是具有2至20个碳原子的二价亚烷基的结构，X和Y独立地是二价连接部分或单键，TsO - 是甲苯磺酸酯，和 Z是保护组。
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2.发明授权Process for the preparation of nonracemic syn-1-(4-hydroxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol compounds 失效制备非内酯顺-1-（4-羟基 - 苯基）-2-（4-羟基-4-苯基 - 哌啶-1-基）-1-丙醇化合物的方法公开(公告)号：US06743921B2
公开(公告)日：2004-06-01
申请号：US10057826
申请日：2002-01-24
IPC分类号： C07D21152
CPC分类号： C07F15/0053 , B01J31/1805 , B01J31/226 , B01J31/24 , B01J31/2409 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07B2200/07 , C07C29/143 , C07C29/145 , C07D211/52 , C07D277/24 , C07D307/44 , C07D333/16 , C07D333/56 , C07F9/3813
摘要： The present invention provides a process for the preparation of a nonracemic diastereomer of 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanol by hydrogenation of a corresponding nonracemic 1-(4-benzoxy-phenyl)-2-(4-hydroxy-4-phenyl-piperidin-1-yl)-1-propanone using a catalyst system comprising ruthenium, a nonracemic diphosphine ligand, a bidentate amine ligand selected from amino-thioethers and achiral diamines, and a base.
摘要翻译： 本发明提供了通过相应的氢化制备1-（4-苯氧基 - 苯基）-2-（4-羟基-4-苯基 - 哌啶-1-基）-1-丙醇的非水性非对映异构体的方法 使用包含钌，非质子二膦配体，二齿胺配位体的催化剂体系的非芳香性1-（4-苯氧基 - 苯基）-2-（4-羟基-4-苯基 - 哌啶-1-基）-1-丙酮 氨基 - 硫醚和非手性二胺，以及碱。
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公开(公告)号：US4661662A
公开(公告)日：1987-04-28
申请号：US782378
申请日：1985-09-30
IPC分类号： H01H31/00
CPC分类号： H01H31/00
摘要： A new and improved apparatus is provided to permit a live or hot electrical power line to be cut in the field for line service or other purposes. The apparatus is connected at each end to the line at positions spanning the site of the cut. The attached end portions are then moved closer to each other, easing the tension on the portion of the line to be cut. The apparatus is then connected to the live line with jumper cables, forming a parallel electric circuit. The line is then cut and a cut end tied back. Flow of current through the apparatus is broken. An interrupter in the apparatus suppresses any arc which may tend to form.
摘要翻译： 提供了一种新的和改进的装置，以允许现场或热电力线在现场切割以用于线路服务或其他目的。 该设备在每一端连接到跨越切割部位的位置处。 然后将附接的端部彼此靠近移动，从而减轻待切割的线的部分上的张力。 然后将该装置用跳线连接到带电线，形成并联电路。 然后将线切割并将剪切端绑回。 通过设备的电流流过。 设备中的断路器抑制可能趋于形成的任何电弧。
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公开(公告)号：US20090203901A1
公开(公告)日：2009-08-13
申请号：US12378363
申请日：2009-02-12
IPC分类号： C07D487/04 , C07C211/45 , C07C233/33 , C07D243/24
CPC分类号： C07D243/24 , C07C221/00 , C07C237/04 , C07D243/28 , C07D487/04 , C07C225/22
摘要： The present invention provides innovative strategies for synthesizing pyrazole ring-functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha-aminoamidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies.
摘要翻译： 本发明提供用于合成吡唑环官能化苯并二氮杂酮的创新策略。 用于形成α-氨基二苯甲酮中间体的替代中间体和高转化策略涉及芳族酰化，负电离离子基团与胺的置换，然后是N-位移策略以产生具有伯胺官能团的所需α-氨基二苯甲酮的组合。 然后提供反应策略，以高产率和方便的反应策略将α-氨基二苯甲酮转化为α-氨基氨基二苯甲酮中间体。 然后将这些α-氨基氨基二苯甲酮中间体转化为苯并二氮杂酮。 然后通过一系列创新的中间体和/或反应策略将这些苯并二氮杂酮转化成吡唑环官能化的苯并二氮杂酮。
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公开(公告)号：US06806378B2
公开(公告)日：2004-10-19
申请号：US10153421
申请日：2002-05-21
IPC分类号： C07F1500
CPC分类号： C07F15/0053 , B01J31/1805 , B01J31/226 , B01J31/24 , B01J31/2409 , B01J2231/643 , B01J2531/821 , C07B53/00 , C07B2200/07 , C07C29/143 , C07C29/145 , C07D211/52 , C07D277/24 , C07D307/44 , C07D333/16 , C07D333/56 , C07F9/3813
摘要： The present invention provides a catalyst system and a process for the preparation of a nonracemic chiral alcohol by hydrogenation of a ketone using the catalyst system, wherein the catalyst system comprises ruthenium, a nonracemic chiral diphosphine ligand, an amino-thioether ligand, and a base.
摘要翻译： 本发明提供催化剂体系和通过使用催化剂体系氢化酮来制备非糖化手性醇的方法，其中催化剂体系包含钌，非手性二膦配体，氨基硫醚配体和碱 。
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公开(公告)号：US20080161564A1
公开(公告)日：2008-07-03
申请号：US12004204
申请日：2007-12-20
IPC分类号： C07D241/10
CPC分类号： C07D319/08 , C07D241/20
摘要： The present invention advantageously provides ketal functional compounds that can be strong electrophiles under conditions compatible with ketal groups, are stable, crystalline solids at room temperature, and are much safer to handle than ketal iodides. The present invention accomplishes by incorporating aromatic sulfonyl moieties into ketal functional materials. The compounds are useful starting materials or intermediates in the synthesis of more complex organic molecules.
摘要翻译： 本发明有利地提供缩酮官能化合物，其在与缩酮基团相容的条件下可以是强亲电体，在室温下是稳定的，结晶固体，并且比酮碘化物更安全。 本发明通过将芳香族磺酰部分引入缩酮功能材料来实现。 这些化合物是合成更复杂有机分子的有用起始原料或中间体。
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7.发明申请Reduction methodologies for converting ketal acids, salts, and esters to ketal alcohols 审中-公开将缩酮酸，盐和酯转化为缩酮醇的还原方法公开(公告)号：US20080161563A1
公开(公告)日：2008-07-03
申请号：US12004191
申请日：2007-12-20
IPC分类号： C07D241/20 , C07D319/08
CPC分类号： C07D319/08 , C07D241/26
摘要： The present invention relates to methods of reducing ketal acids, salts and esters to form corresponding ketal alcohols. More particularly, the reducing methods convert the ketal acids, salts, or esters to ketal alcohols by using a reducing agent that comprises a hydride that comprises one or more alkoxy moieties. The ketal alcohol is prepared in a hydrophobic reagent. This is purified by washing the hydrophobic reagent with one or more water washes. Because the ketal alcohol has some water solubility, the water washes are back-extracted with a hydrophobic solvent to recover additional ketal alcohol from such one or more water washes. The alcohol products are useful in many applications such as intermediates in the synthesis of pharmacologically important molecules.
摘要翻译： 本发明涉及还原缩酮酸，盐和酯以形成相应的缩酮醇的方法。 更具体地，还原方法通过使用包含包含一个或多个烷氧基部分的氢化物的还原剂将缩酮酸，盐或酯转化为缩酮醇。 缩酮醇在疏水性试剂中制备。 这通过用一次或多次洗涤水洗涤疏水性试剂来纯化。 因为缩酮醇具有一定的水溶性，所以用疏水性溶剂反冲洗水洗，从这种一次或多次水洗中回收另外的缩酮醇。 醇产物在许多应用中是有用的，例如合成药理学重要分子的中间体。
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公开(公告)号：US5618958A
公开(公告)日：1997-04-08
申请号：US695143
申请日：1996-08-08
IPC分类号： C07F13/00
CPC分类号： C07F13/005 , Y02P20/582
摘要： A novel catalyst comprising the formula:LRE(O)nwhereinL is selected from the group consisting of(a) (R.sub.1)(AL)wherein R.sub.1 is an alkyl side chain containing at least one carbon-rhenium covalent bond, andAL is a molecule having C.sub.2 to C.sub.50, and has at least one hetero atom selected from the group consisting of N, O, S, and P wherein there is at least one hetero-rhenium dative bond, and has at least one chiral center. and(b) R.sub.AL is a straight or branched chain alkyl or arylalkyl group containing C.sub.2 to C.sub.50 and containing at least one heteroatom selected from the group consisting of N, O, S, and P, with the proviso that said alkyl group contains at least one carbon-rhenium covalent bond and at least one hetero-rhenium dative bond, and has at least one chiral center:and n is an integer which is 2, 3, 4, or 5 and which has utility in areas such as epoxidation of olefins.
摘要翻译： 一种新型催化剂，其包含式LRE（O）n，其中L选自（a）（R1）（AL）其中R1是含至少一个碳 - 铼共价键的烷基侧链，AL是 具有C 2至C 50的分子，并且具有至少一个选自N，O，S和P的杂原子，其中存在至少一个异铼双键，并且具有至少一个手性中心。 和（b）RAL是含有C 2至C 50的直链或支链烷基或芳基烷基，并且含有至少一个选自N，O，S和P的杂原子，条件是所述烷基至少包含 一个碳 - 铼共价键和至少一个异铼双键，并且具有至少一个手性中心：和n是2,3,4或5的整数，并且其在例如烯烃的环氧化 。
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公开(公告)号：US5574196A
公开(公告)日：1996-11-12
申请号：US395267
申请日：1995-02-28
IPC分类号： C07C29/48 , C07C31/125 , C07C35/06 , C07C35/21
CPC分类号： C07C29/48 , C07C2101/08 , C07C2102/28
摘要： A process for preparing tertiary alkanols which comprises the step of oxidizing with ozone a saturated hydrocarbon having a tertiary carbon center in the presence of a carboxylic acid and for a sufficient period of time and at suitable temperature and pressure to form said alkanols.
摘要翻译： 一种制备叔链烷醇的方法，其包括在羧酸存在下用臭氧氧化具有叔碳中心的饱和烃并在合适的温度和压力下充分形成所述链烷醇的步骤。
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10.发明授权
公开(公告)号：US5491265A
公开(公告)日：1996-02-13
申请号：US395266
申请日：1995-02-28
CPC分类号： C07C29/48 , C07C45/511 , C07C71/00 , C07C2101/08
摘要： A process for preparing 6-chloro-2-hexanone which comprises the steps of (a) oxidizing methylcyclopentane with ozone in the presence of a carboxylic acid and for a sufficient period of time to form 1-methylcyclopentanol; (b) reacting said 1-methylcyclopentanol with a suitable amount of an alkali metal hypochlorite in the presence of a carboxylic acid to form 1-methylcyclopentyl hypochlorite; and (c) heating said 1-methylcyclopentyl hypochlorite for a sufficient period of time to form 6-chloro-2-hexanone.
摘要翻译： 一种制备6-氯-2-己酮的方法，其包括以下步骤：（a）在羧酸存在下用臭氧氧化甲基环戊烷并持续足够的时间以形成1-甲基环戊醇; （b）在羧酸存在下使所述1-甲基环戊醇与适量的碱金属次氯酸盐反应，形成1-甲基环戊基次氯酸盐; 和（c）将所述1-甲基环戊基次氯酸盐加热足够的时间以形成6-氯-2-己酮。
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