CAS: 109384-19-2; Tert-Butyl 4-Hydroxypiperidine-1-Carboxylate

该化合物是属于管道衍生物一类的化学化合物,这种化合物具有管状环,是六人组成的饱和含氮的乙型环,其特点是存在一种氢氧基(-OH)和一种用乙丁醇浸泡的碳oxylic ephyldy modie,该组增加了分子的脂性,有可能影响其溶解性和再活性.该化合物由于其结构特性,可能有助于生物活动,经常用于有机合成和医药化学中.该组可参与氢的结合,而管状环可作为一个基本场所,使其在合成各种药品和农用化学物时成为多功能的中间体.应当与任何化学物质一起观察安全和处理预防措施,以减少其使用的风险.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

4-HYDROXYPIPERIDINE tert-butyl dicarbonatedi-tert-butyl dicarbonate N-tert-butyloxycarbonylpiperidin-4-one t-butyl piperidinecarboxylateN-tert-butyloxycarbonylpiperidin-4-one 4-(N-t-Butoxycarbonyl-4-piperidinyloxy)-2-hydroxybenzoic acid methyl ester tert-butyl 4-(tosyloxy)piperidin-1-carboxylate 4-(4-Cyano-3-fluoro-phenoxy)-piperidine-1-carboxylic acid tert-butyl ester

合成工艺路线路线简述

  • 合成目标产物 N-Boc-4-Hydroxypiperidine 主要起始原料 N-(Tert-Butoxycarbonyl)-4-Piperidone
  • (文献来源)合成步骤主要原料 N-(Tert-Butoxycarbonyl)-4-Piperidone
4-羟基哌啶置于碳酸二叔丁酯,三乙胺体系中,用 二氯甲烷 用作溶剂,化学反应 21.0H,以100%的收率获得n-Boc-4-羟基哌啶
参考文献:Hydroxamic And Carboxylic Acid Derivatives
标题:Hydroxamic And Carboxylic Acid Derivatives
摘要:具有治疗效用的化合物的公式为(I)B-x-(Ch2)N-cr2R3-cr4R5-coy (I),其中n为0-1;X为s(O)0-2,Y为or1或nhoh;R2和r4独立地为h或从c1-6烷基,C2-6烯基,芳基,C1-6烷基芳基,杂芳基,C1-6烷基杂芳基,杂环烷基,C1-6烷基杂环烷基,环烷基和c1-6烷基环烷基中选择的(可选地用r10取代的)基团;R1,R3和r5独立地为h或c1-6烷基;但不得超过两个r2,R3,R4和r5为h;或cr2R3,Cr4R5和cr2-cr4中的任何一个为杂环烷基或杂环烷基环,可选地用r10取代,或从c1-6烷基,芳基,C1-6烷基芳基,杂芳基和c1-6烷基杂芳基中选择的(可选地用r10取代的)基团;B为通过碳与x相连的杂环烷基(可选地用r6或r7取代),或c1-6烷基杂环烷基(可选地用r6或r7取代),或从c1-8烷基,C2-6烯基和c2-6炔基中选择的(用r6取代的)基团;R6为n(R7)2,Or7,Cor7,C(=nor9)R7,Nr7R8,S(O)0-2R9或so2N(R7)2;R7为h或从c1-6烷基,芳基,C1-6烷基芳基,杂芳基,C1-6烷基杂芳基,环烷基,C1-6烷基环烷基,杂环烷基和c1-6烷基杂环烷基中选择的基团,其中所述基团可选地用r9,Cor9,So0-2R9,Co2R9,Or9,Conr1R9,Nr1R9,卤素,Cn,So2Nr1R9或no2取代,对于每种情况的n(R7)2,R7基团相同或不同,或n(R7)2为可选地用r9,Cor9,So0-2R9,Co2R9,Or9,Conr1R9,Nr1R9,卤素,Cn,So2Nr1R9或no2取代的杂环烷基;R8为cor7,Con(R7)2,Co2R9或so2R9;R9为c1-6烷基,芳基,C1-6烷基芳基,杂芳基或c1-6烷基杂芳基;R10为or7,Cor7,Co2R1,Con(R7)2,Nr7R8,S(O)0-2R9,So2N(R7)2,Cn,卤素或环亚咪唑基(可选地用r1取代);及其盐,溶剂化合物,水合物,N-氧化物,保护氨基,保护羧基和保护羟胺衍生物.

专利信息


专利号:WO-9731891-A1
优先权日:1996-03-01
标 题:Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile
发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M
权利人:MERCK & CO INC; LYNCH JOSEPH E; SHI YAO JUN; WELLS KENNETH M
摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人:ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-8399502-B2
优先权日:2008-09-17
标 题 :Analogs of indole-3-carbinol and their use as agents against infection
发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN
权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT
摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.

专利号:US-9650337-B2
优先权日:2013-02-14
标 题 :Method of synthesising 4-piperidin-4-yl-benzene-1,3-diol and the salts of same and novel compound tert-butyl 4-(2,4-dihydroxy-phenyl)-4-hydroxy-piperidine-1-carboxylate
发明人:BOITEAU JEAN-GUY; MUSICKI BRANISLAV
权利人:GALDERMA RES & DEV
摘要:A method is described for the synthesis of 4-piperidin-4-yl-benzene-1,3-diol of the following formula (I): n nand the pharmaceutically acceptable salts thereof. Also described, is tert-butyl 4-(2,4-dihydroxy-phenyl)-4-hydroxy-piperidine-1-carboxylate as a novel intermediate compound

专利号:US-5777123-A
优先权日:1996-03-01
标题 :Process for regioselective substitution of trifluorobenzoate or trifluorobenzonitrile
发明人:LYNCH JOSEPH E; SHI YAO-JUN; WELLS KENNETH M
权利人:MERCK & CO INC
摘要:The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

专利号:US-2009118296-A1
优先权日:2005-07-20
标 题:Heteroaromatic Compounds As Inhibitors Of Stearoyl-Coenzyme A Delta-9 Desaturase
发明人:BLACK CAMERON; DESCHENES DENIS; GAGNON MARC; LACHANCE NICOLAS; LEBLANC YVES; LEGER SERGE; LI CHUN SING; OBALLA RENATA M
权利人:MERCK FROSST CANADA LTD
摘要:Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; lipid disorders; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and fatty liver disease.
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合成参考文献


摘要:Li, H.; Mazet, C., Science of Synthesis Knowledge Updates, (2015) 2, 42.
摘要:Nolte, J. C.; Urlacher, V. B., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 36.
摘要:Joosten, A.; Brioche, J., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 24.
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