CAS: 4644-61-5; Ethyl 4-Oxo-3-Piperidinecarboxylate Hydrochloride

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1-苄基-4-哌啶酮-3-羧酸乙酯置于盐酸,Palladium 10% On Activated Carbon,氢气体系中,用 乙醇 作为反应溶剂,40.0 °C,506.66 Kpa 条件下,反应 8.0H,以95%的收率获得产物盐酸-4-哌啶酮-3-羧酸乙酯
参考文献:基于4-苯胺基四氢吡啶并[4,3-D]嘧啶支架的新型抗增殖剂和egfr酪氨酸激酶潜在抑制剂的发现:设计,合成和生物学评估.
标题:基于4-苯胺基四氢吡啶并[4,3-D]嘧啶支架的新型抗增殖剂和egfr酪氨酸激酶潜在抑制剂的发现:设计,合成和生物学评估.
摘要:设计,合成了一系列新颖的4-芳基氨基-6 / 7-取代的5,6,7,8-四氢吡啶并[4,3-D]嘧啶类化合物,它们作为潜在的抗增殖剂和egfr激酶抑制剂具有生物活性被评估.thpps中的n-丙烯酰胺片段和带有取代基的4-苯胺基团都起着关键作用,因为它们对四种癌细胞系(ht29,A549,H460和h1975)具有显着的抗增殖活性.吉非替尼抗性的h1975尤其抑制活性显示更有利的,这可从化合物可以观测到图13B,13C,13N,13O,13P,13R,13S,13U和24C显然.通过抑制egfr和her2激酶,七种化合物(评价13B,13克,13N,13O,13P,13R和13S)显示更强的egfr效力与ic 50 ⩽18纳米,这也可以通过初步对接研究理解13B中与egfr激酶.鉴于原发性sar,双芳基苯胺衍生物(13O,13P,13R和13S)显示出对her2抑制的明显改善,表明它们是潜在的egfr
DOI:10.1016/j.Bmc.2015.05.059

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:CN-109320515-A
优先权日:2018-11-22
标题:A kind of method of asymmetric synthesis of Capromorelin chiral intermediate

专利号:IL-138911-A
优先权日:1995-12-28
标 题:Dipeptide intermediate compound in the synthesis of growth-hormone secretagogues