CAS: 161491-24-3; 1-Tert-Butyl 3-Methyl 4-Oxopiperidine-1,3-Dicarboxylate

相似化合物

3939-01-3 13049-77-9 406212-51-9

上下游产品

4-氧基-哌啶-3-羧酸甲酯 Methyl 4-Oxonipecotate 108554-34-3
N-叔丁氧羰基-4-哌啶酮 N-Tert-Butyloxycarbonylpiperidin-4-One 79099-07-3

📜1-苄基-3-甲氧羰基-4-哌啶酮盐酸盐置于palladium 10% On Activated Carbon,氢气,溶剂黄146,三乙胺体系中,用 甲醇,二氯甲烷,水 用作溶剂,化学反应 31.0H,反应生成N-Boc-4-哌啶酮-3-甲酸甲酯
参考文献:非对映会聚钴催化芳基化全合成 (+/-)-帕罗西汀
标题:非对映会聚钴催化芳基化全合成 (+/-)-帕罗西汀
摘要:报道了帕罗西汀的全合成,其中涉及 3-取代 4-溴-N-Boc-哌啶(boc = 叔丁氧羰基)底物的非对映选择性和非对映会聚钴催化 Sp3-Sp2 偶联反应作为关键步骤.获得了 9:1 的非对映选择性,而涉及构象锁定的 3-取代 4-溴-叔丁基环己烷环的对照实验则以基本上完全的立体选择性进行.
Doi:10.1002/ejoc.201402108

专利信息

专利号:US-6867202-B1
优先权日:1997-06-25
标 题 :Treatment of insulin resistance
发明人：CARPINO PHILIP ALBERT; CHIU CHARLES KWOK-FUNG; PAN LYDIA CODETTA; LEFKER BRUCE ALLEN; TREADWAY JUDITH LEE; ZAWISTOSKI MICHAEL PAUL
权利人:PFIZER
摘要:This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, n n nwhere the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.

专利号:EP-1404682-B1
优先权日:2001-06-29
标题:Method of inhibiting ptp 1b and/or t-cell ptp and/or other ptpases with an asp residue at position 48
发明人：HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL
权利人:NOVO NORDISK AS
摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.

专利号:US-2003064979-A1
优先权日:2001-06-29
标题 :Method of inhibiting PTP 1B and /or T-cell PTP and/or other PTPases with an Asp residue at position 48
发明人：HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL
摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al, Proc Natl Acad Sci USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1 n n n This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.

专利号:WO-2004058727-A1
优先权日:2002-12-20
标题 :Substituted 3,5-dihydro-4h-imidazol-4-ones for the treatment of obesity
发明人：CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA
权利人:BAYER PHARMACEUTICALS CORP; CHEN YUANWEI; O'CONNOR STEPHEN JAMES; GUNN DAVID; NEWCOM JASON; CHEN JIANQING; YI LIN; ZHANG HAI-JUN; HUNYADI LASZLO MATYAS; NATERO REINA
摘要:This invention relates to substituted 3,5-dihydro-4H-imidazol-4-ones compounds which are useful in the treatment of obesity and obesity-related disorders, and as weight-loss and weight-control agents. The invention also provides methods for synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods of using such compositions for inducing weight loss and treating obesity and obesity-related disorders.

专利号:US-8772301-B2
优先权日:2009-12-18
标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
发明人：HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D
权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

专利号:US-6096763-A
优先权日:1995-02-23
标题 :α1a adrenergic receptor antagonists
发明人：HOFFMAN JACOB M; CHANG RAYMOND S L
权利人:MERCK & CO INC
摘要:This invention relates to novel compounds, their synthesis and use as selective α 1a adrenergic receptor antagonists. One application of the compounds is in the treatment of benign prostatic hyperplasia. The compounds are selective in their ability to relax smooth muscle tissue enriched in the α 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.