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公开(公告)号：US4908450A
公开(公告)日：1990-03-13
申请号：US304304
申请日：1989-01-31
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): ##STR1## whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuration (II) over the cis configuration (III) as defined in the following formulae: ##STR2## The preferred reaction conditions include use of a borane complex as the reducing agent and an acidic solvent such as trifuloroacetic acid.
摘要翻译： 通过还原相应的醇（VII），已知的抗抑郁化合物（I）的非对映选择性方法：其中非对映异构体的产物混合物出人意料地且意外地富含 （III）优选的反应条件包括使用硼烷配合物作为还原剂和酸性溶剂如 作为三氟乙酸。
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2.发明授权Stereoselective reaction for hexahydro-6-arylpyrrolo(2,1-A) isoquinolines 失效六氢-6-芳基吡咯并（2,1-A）异喹啉的立体选择性反应
公开(公告)号：US4837328A
公开(公告)日：1989-06-06
申请号：US156063
申请日：1988-02-16
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： A diastereoselective process for known antidepressive compounds (I) via reduction of the corresponding alcohol (VII): ##STR1## whereby the product mixture of diastereomers is surprisingly and unexpectedly rich in the content of the trans configuration (II) over the cis configuration (III) as defined in the following formulae: ##STR2## The preferred reaction conditions include use of a borane complex as the reducing agent and an acidic solvent such as trifluoroacetic acid.
摘要翻译： 通过还原相应的醇（VII），已知的抗抑郁化合物（I）的非对映选择性方法：其中非对映异构体的产物混合物令人惊讶地和出人意料地富含反式构型（II）的含量超过 如下式所定义的顺式构型（III）：优选的反应条件包括使用硼烷络合物作为还原剂和酸性溶剂如三氟乙酸。
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3.发明授权Process for the preparation of chlorosulfate and sulfamate derivatives of 2,3:4,5-bis-O-(1-methylethylidene)-.beta.-D-fructopyranose and (1-methylcyclohexyl)methanol 失效制备2,3,4,5-双-O-（1-甲基亚乙基）-β-D-吡喃葡萄糖和（1-甲基环己基）甲醇的氯磺酸盐和氨基磺酸盐衍生物的方法
公开(公告)号：US5387700A
公开(公告)日：1995-02-07
申请号：US106470
申请日：1993-08-12
IPC分类号： C07C307/02 , C07C303/34 , C07D309/06 , C07D493/04 , C07D493/14 , C07H9/04 , C07D311/78 , C07C309/02 , C07D311/94
CPC分类号： C07D493/04 , C07C303/34 , C07D309/06 , C07D493/14 , C07H9/04
摘要： A process for producing chlorosulfate and sulfamate esters of 2,3:4,5-bis-O-(1-methylethylidene)-.beta.-D-fructopyranose and (1-methylcyclohexyl)methanol is disclosed. The process involves a two step procedure involving in the first step reacting of an alcohol with sulfuryl chloride in the presence of a tertiary or heterocyclic amine base in a solvent selected from the group consisting of toluene, t-butyl methyl ether or tetrahydrofuran to produce a chlorosulfate intermediate, which is preferably stabilized by an aqueous wash and/or treatment with a base, and in the second step reacting of the resulting intermediate with an amine in a solvent selected from the group consisting of t-butyl methyl ether, tetrahydrofuran and lower alkanol.
摘要翻译： 公开了一种制备2,3,4,5-双-O-（1-甲基亚乙基）-β-D-吡喃葡萄糖和（1-甲基环己基）甲醇的氯代硫酸盐和氨基磺酸酯的方法。 该方法涉及两步法，该方法包括在叔胺或杂环胺碱存在下，在选自甲苯，叔丁基甲基醚或四氢呋喃的溶剂中，将醇与磺酰氯反应的第一步骤，以产生 氯代硫酸盐中间体，其优选通过水性洗涤和/或用碱处理而稳定，并且在第二步中，将得到的中间体与胺在选自叔丁基甲基醚，四氢呋喃和低级 链烷醇
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![Process for preparing [S-(R*,S*)]-&bgr;-[[[1-[1-oxo-3(4-piperidinyl)propyl]-3-piperidinyl]carbonyl]amino]-3-pyridinepropanoic acid and derivatives](/abs-image/US/2003/02/04/US06515130B1/abs.jpg.150x150.jpg)
4.发明授权Process for preparing [S-(R*,S*)]-&bgr;-[[[1-[1-oxo-3(4-piperidinyl)propyl]-3-piperidinyl]carbonyl]amino]-3-pyridinepropanoic acid and derivatives 有权制备[S-（R *，S *）]-β - [[[1- [1-氧代-3（4-哌啶基）丙基] -3-哌啶基]羰基]氨基] -3-吡啶丙酸和 衍生品公开(公告)号：US06515130B1
公开(公告)日：2003-02-04
申请号：US09532375
申请日：2000-03-21
申请人： Judith H. Cohen , Michael Justus , Cynthia A. Maryanoff , Armin Rössler , Fridtjof Schröder , Kirk L. Sorgi , Frank J. Villani, Jr. , Christian Weh
发明人： Judith H. Cohen , Michael Justus , Cynthia A. Maryanoff , Armin Rössler , Fridtjof Schröder , Kirk L. Sorgi , Frank J. Villani, Jr. , Christian Weh
IPC分类号： C07D40112
CPC分类号： C07D401/14
摘要： A process for preparing a compound of formula I wherein R1 and R2 are independently selected from the group consisting of hydrogen, lower alkyl and halogen
摘要翻译： 制备式I化合物的方法，其中R1和R2独立地选自氢，低级烷基和卤素
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公开(公告)号：US5952187A
公开(公告)日：1999-09-14
申请号：US565143
申请日：1995-12-01
IPC分类号： G01N33/53 , C07H9/04 , C07H15/26 , C07K16/44 , C12N5/10 , C12N15/02 , C12P21/08 , C12R1/91 , G01N33/94 , G01N33/533 , C12N9/96 , G01N33/535
CPC分类号： C07H9/04 , G01N33/9473 , Y10S436/815
摘要： The present invention provides a topiramate immunoassay and reagents for use in the immunoassay. In particular, topiramate is derivatized at the sulfamate moiety or the 9-carbon or 10-carbon methyl group of topiramate to add a label bound directly or through a linking group for use as a tracer (competitive analyte analog) or to add a linking group bound to a carrier for use as an immunogen to induce anti-topiramate antibodies. Immunoassay methods and kits are also provided.
摘要翻译： 本发明提供托吡酯免疫测定法和用于免疫测定的试剂。 特别地，托吡酯衍生化在托吡酯的氨基磺酸酯部分或9-碳或10-碳甲基上，以添加直接或通过连接基团结合的标记，用作示踪剂（竞争性分析物类似物）或添加连接基团 结合载体用作免疫原诱导抗托吡酯抗体。 还提供免疫测定方法和试剂盒。
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公开(公告)号：US08309720B2
公开(公告)日：2012-11-13
申请号：US12459229
申请日：2009-06-29
申请人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
发明人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
IPC分类号： C07D211/06 , C07D211/30
CPC分类号： C07D401/12 , C07C211/22 , C07C211/26 , C07D211/22 , C07D211/26
摘要： The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
摘要翻译： 本发明涉及制备用作合成组胺H 4受体调节剂的中间体的取代嘧啶衍生物的方法，以及H4调节剂合成中的中间体。
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7.发明申请PROCESS FOR THE PREPARATION OF PIPERAZINYL AND DIAZEPANYL BENZAMIDE DERIVATIVES 有权制备哌嗪和二氮茚衍生物衍生物的方法公开(公告)号：US20080171870A1
公开(公告)日：2008-07-17
申请号：US11953262
申请日：2007-12-10
申请人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
发明人： Anusuya Choudhury , Jeffrey S. Grimm , Kirk L. Sorgi , David Palmer , Jing Liu
IPC分类号： C07D413/00 , C07D295/00
CPC分类号： C07D413/10 , C07D241/04 , C07D401/10 , C07D403/10 , Y02P20/55
摘要： The present invention is directed to a novel process for the preparation of piperazinyl and diazepanyl benzamide derivatives, useful for the treatment of disorders and conditions mediated by a histamine receptor, preferably the H3 receptor.
摘要翻译： 本发明涉及用于制备哌嗪基和二氮杂环庚烷基苯甲酰胺衍生物的新方法，其可用于治疗由组胺受体介导的病症和病症，优选H3受体。
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公开(公告)号：US5977302A
公开(公告)日：1999-11-02
申请号：US195049
申请日：1998-11-18
申请人： David C. Palmer , Ahmed Abdel-Magid , Michael S. Breslav , Urs P. Eggmann , Bruce Harris , Mark L. Haslego , Kirk L. Sorgi
发明人： David C. Palmer , Ahmed Abdel-Magid , Michael S. Breslav , Urs P. Eggmann , Bruce Harris , Mark L. Haslego , Kirk L. Sorgi
CPC分类号： C07K5/0815 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K7/23 , Y02P20/55
摘要： A liquid phase process for preparing GnRH peptide analogs of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)-AA.sub.5 -AA.sub.6 AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2Formula 1which comprises:(a) reacting a peptide of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -Xwhere T is (P.sub.2)AA4 orP.sub.2 and X is AA.sub.7 --OH or is --OH, with a peptide of the formula:X'-AA.sub.8 -Pro-AA.sub.10 -NH.sub.2or acid-addition salt form thereof, where X' is AA.sub.7 when X is absent and X' selected from P-Ala, Gly, GABA, the D- and L- isomers of Ala, amino isobutyric acid, 6-amino-hexanoic acid, Ser, Thr, His, Tyr, Asn, and Gln' is absent when X is AA.sub.7 --OH;in a liquid reaction medium in the presence of a peptide coupling reagent and a strong organic amine base to obtain a product of the formula:T-(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2(b) removing the P.sub.2 protecting group at the N-terminus, and(c) reacting the product of step (b) or an acid addition salt thereof, with a peptide of the formula:G-AA.sub.1 -(R.sub.1)D-Phe-AA.sub.3 -T'or acid-addition salt form thereof, where T' is AA.sub.4 --OH when T is absent and is absent when T is P2-AA.sub.4, in a liquid reaction medium to obtain a GnRH peptide of the formula:G-AA.sub.1 -(A)D-Phe-AA.sub.3 -AA.sub.4 -(R.sub.2)AA.sub.5 -AA.sub.6 -AA.sub.7 -AA.sub.8 -Pro-AA.sub.10 -NH.sub.2.
摘要翻译： 用于制备下式的GnRH肽类似物的液相方法：G-AA1-（A）D-Phe-AA3-AA4-（R2）-AA5-AA6AA7-AA8-Pro-AA10-NH2式1，其包含：（a ）使下式的肽与下式的肽反应：其中T是（P2）AA4或P2，X是AA7-OH或-OH的式（T-（R2）AA5-AA6-X）肽与下式的肽反应：X'-AA8-Pro -AA10-NH2或其酸加成盐形式，其中当X不存在时X'为AA 7，X'选自P-Ala，Gly，GABA，Ala的D-和L-异构体，氨基异丁酸， 当X是AA7-OH时，氨基己酸，Ser，Thr，His，Tyr，Asn和Gln'不存在; 在液体反应介质中，在肽偶联剂和强有机胺碱的存在下，得到下式的产物：（（R 2）AA 5 -A AA 6 -A AA 7 -A AA 8 -Pro-AA 10 -NH 2（b） P2保护基团，和（c）使步骤（b）的产物或其酸加成盐与下式的肽反应：G-AA1-（R1）D-Phe-AA3-T' 或其酸加成盐形式，其中当T不存在时T'为AA4-OH，当T为P2-AA4时不存在，在液体反应介质中得到G-AA1 - （A）的GnRH肽， D-Phe-AA3-AA4-（R2）AA5-AA6-AA7-AA8-Pro-AA10-NH2。
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公开(公告)号：US20100004450A1
公开(公告)日：2010-01-07
申请号：US12459229
申请日：2009-06-29
申请人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
发明人： Sergio Cesco-Cancian , Hongfeng Chen , Jeffrey S. Grimm , Neelakandha S. Mani , Christopher M. Mapes , David C. Palmer , Daniel J. Pippel , Kirk L. Sorgi , Tong Xiao
IPC分类号： C07D401/12 , C07D211/22 , C07D211/26
CPC分类号： C07D401/12 , C07C211/22 , C07C211/26 , C07D211/22 , C07D211/26
摘要： The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H4 receptor modulators, and to intermediates in H4 modulator synthesis.
摘要翻译： 本发明涉及制备用作合成组胺H 4受体调节剂的中间体的取代嘧啶衍生物的方法，以及H4调节剂合成中的中间体。
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公开(公告)号：US08278446B2
公开(公告)日：2012-10-02
申请号：US11766257
申请日：2007-06-21
IPC分类号： C07D239/48 , C07D239/50 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D413/04 , C07D417/12
摘要： The present invention is directed to a process for chemoselective substitution on a halopyrimidine carboxaldehyde having multiple reactive sites and subsequent stereoselective oxime formation.
摘要翻译： 本发明涉及一种在具有多个反应位点和随后的立体选择性肟形成的卤代嘧啶甲醛上进行化学选择性取代的方法。
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