• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利：CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法，用中文像聊天一样搜索，搜遍4000万医学文献。AI智能推荐，让科研检索更轻松。

立即免费搜索

文件翻译

保留排版，准确专业，支持PDF/Word/PPT等文件格式，支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述，25分钟生成高质量综述，智能提取关键信息，辅助科研写作。

立即免费体验

2,4-二取代哌啶的非对映选择性合成：药物发现的骨架

A diastereoselective synthesis of 2,4-disubstituted piperidines: scaffolds for drug discovery.

作者信息

Watson P S, Jiang B, Scott B

机构信息

Dupont Pharmaceuticals Company, Route 141 and Henry Clay Road, Wilmington, Delaware 19880, USA.

出版信息

Org Lett. 2000 Nov 16;2(23):3679-81. doi: 10.1021/ol006589o.

DOI:10.1021/ol006589o
PMID:11073674
Abstract

A method for the diastereoselective synthesis of 2,4-disubstituted piperidines has been developed which enables the complete control of reaction selectivity merely by changing the order of the reaction sequence. These targets provide convenient platforms for drug discovery which contain easily modified points of diversity.

摘要

已开发出一种非对映选择性合成2,4-二取代哌啶的方法，该方法仅通过改变反应顺序就能完全控制反应选择性。这些目标化合物为药物研发提供了便利的平台，其中包含易于修饰的多样性位点。

相似文献

1
A diastereoselective synthesis of 2,4-disubstituted piperidines: scaffolds for drug discovery.2,4-二取代哌啶的非对映选择性合成：药物发现的骨架
Org Lett. 2000 Nov 16;2(23):3679-81. doi: 10.1021/ol006589o.
2
Enantiocontrolled synthesis of 2,6-disubstituted piperidines by desymmetrization of meso-eta-(3,4,5)-dihydropyridinylmolybdenum complexes. application to the total synthesis of (-)-dihydropinidine and (-)-andrachcinidine.通过内消旋-η-(3,4,5)-二氢吡啶基钼配合物的去对称化对映选择性合成2,6-二取代哌啶。应用于(-)-二氢哌啶和(-)-山油柑碱的全合成。
J Am Chem Soc. 2003 Mar 12;125(10):2878-9. doi: 10.1021/ja029537y.
3
Access to 2,6-disubstituted piperidines: control of the diastereoselectivity, scope, and limitations. Applications to the stereoselective synthesis of (-)-solenopsine A and alkaloid (+)-241D.获得 2,6-二取代哌啶：控制非对映选择性、范围和限制。在 (-)-solenopsine A 和生物碱 (+)-241D 的立体选择性合成中的应用。
J Org Chem. 2013 Mar 15;78(6):2511-26. doi: 10.1021/jo302712f. Epub 2013 Feb 28.
4
Diastereoselective access to nonracemic 2-cis-substituted and 2,6-cis-disubstituted piperidines.非对映选择性合成 2-顺式取代和 2,6-顺式二取代的非手性哌啶。
Org Lett. 2011 Dec 2;13(23):6292-5. doi: 10.1021/ol202796w. Epub 2011 Nov 8.
5
Furanyl cyclic amines: a diastereoselective synthesis of 2,6-syn-disubstituted piperidines under thermodynamic control.呋喃基环胺：在热力学控制下立体选择性合成 2,6-顺式二取代哌啶。
Org Biomol Chem. 2012 Mar 28;10(12):2392-4. doi: 10.1039/c2ob07008a. Epub 2012 Feb 20.
6
Enantioselective synthesis of cis- and trans-3,5-disubstituted piperidines. Synthesis of 20S- and 20R-dihydrocleavamine.顺式和反式3,5-二取代哌啶的对映选择性合成。20S-和20R-二氢裂解胺的合成。
Org Lett. 2003 Aug 21;5(17):3139-42. doi: 10.1021/ol035199+.
7
A diastereoselective intramolecular hydroamination approach to the syntheses of (+)-, (+/-)-, and (-)-pinidinol.
J Org Chem. 2001 Jun 15;66(12):4344-7. doi: 10.1021/jo015603n.
8
Highly diastereoselective arylations of substituted piperidines.高非对映选择性的取代哌啶芳基化反应。
J Am Chem Soc. 2011 Apr 6;133(13):4774-7. doi: 10.1021/ja201008e. Epub 2011 Mar 9.
9
Directed functionalization of 1,2-dihydropyridines: stereoselective synthesis of 2,6-disubstituted piperidines.1,2 - 二氢吡啶的定向官能团化：2,6 - 二取代哌啶的立体选择性合成
Chem Commun (Camb). 2014 Jul 4;50(52):6883-5. doi: 10.1039/c4cc02220c.
10
A regio- and diastereoselective intramolecular nitrone cycloaddition for practical 3- and 2,3-disubstituted piperidine synthesis from gamma-butyrolactone.一种用于从γ-丁内酯实际合成3-和2,3-二取代哌啶的区域和非对映选择性分子内硝酮环加成反应。
J Org Chem. 2009 Jan 2;74(1):254-63. doi: 10.1021/jo8018285.

引用本文的文献

1
Selective synthesis of -dihalopiperidines and 4-halo-1,2,3,6-tetrahydropyridines from halogen substituted homoallylic benzenesulfonamides and aldehydes.从卤素取代的高烯丙基苯磺酰胺和醛选择性合成α-二卤代哌啶和4-卤代-1,2,3,6-四氢吡啶。
RSC Adv. 2025 Jun 23;15(27):21257-21268. doi: 10.1039/d5ra03630e.
2
Designing Cyclic Nitrogen-Bridged Sulfonamides with Anti-Cancer Activity.设计具有抗癌活性的环状氮桥连磺酰胺
ChemMedChem. 2025 Aug 2;20(15):e202400936. doi: 10.1002/cmdc.202400936. Epub 2025 May 14.
3
Synthesis, crystal structure, Hirshfeld surface analysis, DFT and NBO study of ethyl 1-(4-fluoro-phen-yl)-4-[(4-fluoro-phen-yl)amino]-2,6-diphenyl-1,2,5,6-tetra-hydro-pyridine-3-carboxyl-ate.
1-(4-氟苯基)-4-[(4-氟苯基)氨基]-2,6-二苯基-1,2,5,6-四氢吡啶-3-羧酸乙酯的合成、晶体结构、 Hirshfeld表面分析、密度泛函理论及自然键轨道研究
Acta Crystallogr E Crystallogr Commun. 2023 Sep 8;79(Pt 10):877-882. doi: 10.1107/S205698902300748X. eCollection 2023 Oct 1.
4
Application of a novel deep eutectic solvent as a capable and new catalyst for the synthesis of tetrahydropyridines and 1,3-thiazolidin-4-ones.新型深共晶溶剂作为一种有能力的新型催化剂在合成四氢吡啶和 1,3-噻唑烷-4-酮中的应用。
Sci Rep. 2023 Apr 10;13(1):5804. doi: 10.1038/s41598-023-32882-0.
5
3-Chloro-3-methyl-2,6-diarylpiperidin-4-ones as Anti-Cancer Agents: Synthesis, Biological Evaluation, Molecular Docking, and In Silico ADMET Prediction.3-氯-3-甲基-2,6-二芳基哌啶-4-酮类化合物作为抗癌剂：合成、生物评价、分子对接和计算机 ADMET 预测。
Biomolecules. 2022 Aug 8;12(8):1093. doi: 10.3390/biom12081093.
6
attenuated derangement in renal-cardiac function, redox status, lipid profile and reduced TNF-α, interleukins-2, 6 and 8 in high salt diet fed rats.高盐饮食喂养的大鼠肾心功能、氧化还原状态、血脂水平的紊乱减轻，肿瘤坏死因子-α、白细胞介素-2、6和8水平降低。
Heliyon. 2021 Oct 1;7(10):e08106. doi: 10.1016/j.heliyon.2021.e08106. eCollection 2021 Oct.
7
Synthesis and Antimalarial Activity of 1,4-Disubstituted Piperidine Derivatives.1,4-二取代哌啶衍生物的合成及抗疟活性。
Molecules. 2020 Jan 11;25(2):299. doi: 10.3390/molecules25020299.
8
Metallaphotoredox-Catalyzed Cross-Electrophile C-C Coupling of Aliphatic Bromides.金属光氧化还原催化的脂肪族溴化物的交叉电偶 C-C 偶联反应。
J Am Chem Soc. 2018 Dec 19;140(50):17433-17438. doi: 10.1021/jacs.8b12025. Epub 2018 Dec 10.
9
Crystal structure of 4-meth-oxy--(piperidine-1-carbono-thio-yl)benzamide.4-甲氧基-（哌啶-1-碳硫酰基）苯甲酰胺的晶体结构
Acta Crystallogr E Crystallogr Commun. 2017 Sep 25;73(Pt 10):1530-1533. doi: 10.1107/S2056989017013317. eCollection 2017 Oct 1.
10
Rhodium(I)-Complexes Catalyzed 1,4-Conjugate Addition of Arylzinc Chlorides to N-Boc-4-pyridone.铑（I）配合物催化芳基氯化锌与N-Boc-4-吡啶酮的1,4-共轭加成反应。
Molecules. 2017 May 1;22(5):723. doi: 10.3390/molecules22050723.