Synlett最新文献 - Book学术

Iron Porphyrin Catalysts Induce Stereospecific Glycosylation with Glycal Epoxides. 铁卟啉催化剂诱导环氧甘油立体特异性糖基化。

IF 1.4 4区化学

Synlett Pub Date : 2026-04-30 DOI: 10.1055/a-2861-7444

Hao Xu, Dakang Zhang, Xiao-Wen Zhang, Le Yin, Zixiang Jiang, Pinzhi Wang, Haoyu Yang, David K Vapnek, Thomas J Showstead

引用次数: 0

Stable Vicinal Bisketene Equivalents for Aryne Diels-Alder Reactions. Aryne Diels-Alder反应的稳定邻苯二烯当量。

IF 1.4 4区化学

Synlett Pub Date : 2026-01-15 DOI: 10.1055/a-2779-2027

Jessica E Budwitz, Christopher G Newton

引用次数: 0

TiCl₄-Promoted Intramolecular Friedel-Crafts Cyclization of α-Keto-phenylbutanoates: Synthesis of Substituted Indane and Indene Derivatives. ticl4促进的α-酮苯丁酸酯的分子内Friedel-Crafts环化：取代茚及其衍生物的合成。

IF 1.4 4区化学

Synlett Pub Date : 2026-01-01 Epub Date: 2025-10-02 DOI: 10.1055/a-2698-1214

Arun K Ghosh, Tristan John McDonald

引用次数: 0

Asymmetric Isochalcogenourea-Catalyzed Synthesis of 3,4-Dihydropyrans via (4+2)-Cycloadditions of Ethyl But-3-ynoate with Michael Acceptors. 不对称异硫原脲催化合成3,4-二氢吡喃的（4+2）环加成-3-乙酸乙酯与Michael受体。

IF 1.4 4区化学

Synlett Pub Date : 2025-12-01 Epub Date: 2025-08-18 DOI: 10.1055/a-2659-8340

Mario Hofer, Magdalena Piringer, Anna Scheucher, Lukas S Vogl, Mario Waser

引用次数: 0

Inverting the Conventional Site Selectivity of Cross-Coupling of 2,4-Dichloropyrimidines. 2,4-二氯嘧啶交叉偶联传统位点选择性的逆转。

IF 1.4 4区化学

Synlett Pub Date : 2025-11-05 DOI: 10.1055/a-2710-1288

Oliver D Jackson, Sharon R Neufeldt

引用次数: 0

Synthesis and evaluation of N-arylsulfonylated succinimides as activity-based probes. n -芳基磺酰基琥珀酰亚胺活性探针的合成及评价。

IF 1.4 4区化学

Synlett Pub Date : 2025-10-01 Epub Date: 2025-05-25 DOI: 10.1055/s-0043-1775487

Jo Chvatal, Dat T Nguyen, Alexondra S Xie, William H Parsons

{"title":"Synthesis and evaluation of N-arylsulfonylated succinimides as activity-based probes.","authors":"Jo Chvatal, Dat T Nguyen, Alexondra S Xie, William H Parsons","doi":"10.1055/s-0043-1775487","DOIUrl":"10.1055/s-0043-1775487","url":null,"abstract":"Activity-based protein profiling (ABPP) technology has served as a powerful platform for studying proteins for more than two decades. However, the further growth of this field depends on the development of new probe structures to expand the proportion of the proteome that can be studied using these methods. Inspired by previous reports of succinimide-containing covalent inhibitors for proteases, we synthesized a panel of potential probe structures with a succinimide reactive group and a terminal alkyne tag suitable for subsequent azide-alkyne click chemistry. Members of this panel with an N-arylsulfonyl linker produce labeling of both purified serine proteases as well as proteins in complex cellular lysates. We found that one of these probes labels the human rhomboid protease RHBDL2 at low micromolar concentrations and can be competed with active-site inhibitors. Our studies establish succinimide as a new reactive group for the development of activity-based probes and offer a new chemical tool for studying a class of enzymes with limited functional characterization.","PeriodicalId":22319,"journal":{"name":"Synlett","volume":"36 16","pages":"2603-2608"},"PeriodicalIF":1.4,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12478521/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145207639","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Hydrophilic α-Aryl-α-Diazoamides for Protein Esterification. 亲水性α-芳基-α-重氮酰胺蛋白酯化。

IF 1.4 4区化学

Synlett Pub Date : 2025-10-01 Epub Date: 2025-07-15 DOI: 10.1055/s-0043-1775499

Aniekan Okon, Anton Morgunov, Jinyi Yang, Yana D Petri, Henry R Kilgore, Yanfeng Li, Eric R Strieter, Ronald T Raines

{"title":"Hydrophilic α-Aryl-α-Diazoamides for Protein Esterification.","authors":"Aniekan Okon, Anton Morgunov, Jinyi Yang, Yana D Petri, Henry R Kilgore, Yanfeng Li, Eric R Strieter, Ronald T Raines","doi":"10.1055/s-0043-1775499","DOIUrl":"10.1055/s-0043-1775499","url":null,"abstract":"Bioreversible protein esterification is a simple, customizable, and traceless strategy for the exogenous delivery of proteins into mammalian cells. Enabling this protein delivery strategy are α-aryl-α-diazoamides bearing a tolyl moiety. The aqueous solubility of the ensuing esterified protein is, however, often compromised, which can result in the loss of soluble esterified protein for downstream applications. Here, we undertook a structure-activity relationship campaign to generate hydrophilic diazoamides for use as protein esterification and cellular delivery agents. We find that the careful adjustment of the hydrogen-bond basicity of α-aryl-α-diazoamides is sufficient to engender soluble esterified proteins, as high hydrogen-bond basicity correlates with high aqueous solubility. Importantly, enhancing aqueous solubility of diazoamides should proceed pari passu with preserving their lipophilicity and reactivity towards esterification of carboxylic acids, as the best-performing diazoamide from our study contains an N-acetyl piperazine while retaining the tolyl moiety. Our efforts can inspire new generations of esterified proteins with better solubility.","PeriodicalId":22319,"journal":{"name":"Synlett","volume":"36 17","pages":"2883-2889"},"PeriodicalIF":1.4,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12700464/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"145757544","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Efficient Regioselective Synthesis of Benzimidazoles and Azabenzimidazoles to Enable the Rapid Development of Structure-Activity Relationships for Activation of SLACK Potassium Channels. 高效区域选择性合成苯并咪唑和氮杂苯并咪唑，使SLACK钾通道激活的构效关系快速发展。

IF 1.4 4区化学

Synlett Pub Date : 2025-10-01 Epub Date: 2025-05-23 DOI: 10.1055/a-2586-6260

Paul K Peprah, Brittany D Spitznagel, Yu Du, Dalena Nguyen, C David Weaver, Kyle A Emmitte

{"title":"Efficient Regioselective Synthesis of Benzimidazoles and Azabenzimidazoles to Enable the Rapid Development of Structure-Activity Relationships for Activation of SLACK Potassium Channels.","authors":"Paul K Peprah, Brittany D Spitznagel, Yu Du, Dalena Nguyen, C David Weaver, Kyle A Emmitte","doi":"10.1055/a-2586-6260","DOIUrl":"10.1055/a-2586-6260","url":null,"abstract":"The sodium activated potassium channel known as SLACK (KNa1.1 or Slo2.2) is widely expressed in the central nervous system and represents a potential target for the treatment of several neurological disorders. While much recent progress has been made toward the discovery of small molecule inhibitors of these channels, reports regarding small molecule activators have been scant. Having identified such compounds via a high-throughput screen, we were interested in establishing structure-activity relationships that could serve as the foundation for the design of potent activators of SLACK channels. In this Letter, we describe the implementation of an efficient synthetic approach to the regioselective synthesis of a series of benzimidazole and azabenzimidazoles based on one of our hit compounds. The key step utilizes a one-pot reduction/formylation/condensation reaction of 2-nitro-arylamines. Also presented herein is functional activity for 15 new analogs prepared by this approach and obtained via a thallium-flux assay in cells stably expressing human wild-type SLACK channels. Many of these new analogs demonstrated substantially improved potency relative to the initial hit compound and provide valuable new data that can be utilized in the design of additional derivatives.","PeriodicalId":22319,"journal":{"name":"Synlett","volume":"36 16","pages":"2597-2602"},"PeriodicalIF":1.4,"publicationDate":"2025-10-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC12854702/pdf/","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"146107138","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"OA","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}

引用次数: 0

Iron-Catalyzed Stereoselective Nitrogen Atom Transfer for 1,2-cis-Selective Glycosylation. 铁催化的1,2-顺式选择性糖基化的立体选择性氮原子转移。

IF 1.4 4区化学

Synlett Pub Date : 2025-08-20 DOI: 10.1055/a-2654-5609

Hao Xu, Dakang Zhang, Zixiang Jiang, Le Yin, Spencer I Clark, Pinzhi Wang, Jordan D Lamar, Adam M Cohen

引用次数: 0

Nucleophilic Additions of Organolithium Reagents to Heterocyclic Aldimines. 杂环醛胺中有机锂试剂的亲核加成。

IF 1.4 4区化学

Synlett Pub Date : 2025-08-01 Epub Date: 2025-06-20 DOI: 10.1055/a-2593-6446

Justin Baek, Walker A Hoisington, Evelyn S Galgano, Ethan H Schneider, Timothy J Barker

引用次数: 0