Sodium Trifluoroacetate mediated Copper-Catalyzed aza-Michael addition of α,β-unsaturated olefins with aromatic amines [0.03%]
三氟乙酸钠介导的铜催化芳香胺与α,β-不饱和烯烃的aza-Michael加成反应
S Erfan Masaeli,Mohsen Teimouri,Bhupendra Adhikari et al.
S Erfan Masaeli et al.
We present a sodium trifluoroacetate (CF3CO2Na) mediated copper-catalyzed aza-Michael addition of aromatic amines with activated olefins under mild, aqueous reaction conditions. This simplistic protocol employs a copper catalyst (10 mol%) a...
Nyema M Harmon,Nathaniel R Gehrke,David F Wiemer
Nyema M Harmon
Vinyl bisphosphonates can be readily prepared by condensation of an aromatic aldehyde with the tetraester of a methylenebisphosphonate, and reduction of the resulting olefin is an attractive strategy for the preparation of monoalkyl geminal...
Peng Yu,Wen Zhang,Song Lin
Peng Yu
Radical cascade cyclization reactions provide an efficient method for the construction of polycyclic architectures with multiple stereogenic centers. However, achieving enantioselectivity control of this type of reaction is a challenging ta...
Potassium carbonate-mediated β-selective anomeric O-alkylation with primary electrophiles: Application to the synthesis of glycosphingolipids [0.03%]
碳酸钾介导的主电性体与primary亲电子体的β选择性(anomerical)O烷基化：甘油鞘脂合成中的应用
Ishani Lakshika Hettiarachchi,Fenglang Wu,Maria Stoica et al.
Ishani Lakshika Hettiarachchi et al.
Stereoselective construction of a variety of β-glycosides can be achieved using abundant and inexpensive K2CO3-mediated stereoselective anomeric O-alkylation of sugar lactols with primary electrophiles. In addition, application of this met...
Preparation of β-Hydroxyketones (Aldols) from the Alkylation of O-Silyl Aryl Cyanohydrins with Epoxides [0.03%]
由氰醇酯与环氧乙烷反应制备β-羟基酮（缩醛）
Lissa D Gilreath,Diamond R Melendez,Caylie A McGlade et al.
Lissa D Gilreath et al.
β-Hydroxyketones (aldols) are prepared from the alkylation-deprotection of O-silylated aryl cyanohydrins with epoxides. Key to the success of the method was the suppression of an in situ cyclic imidate formation that occurs upon initial op...
Synthesis of 2,3-Disubstituted Pyrroles by Lewis Acid Promoted Cyclization of N-Sulfonyl Vinylogous Carbamates and Amides [0.03%]
路易斯酸促进的N-磺酰基乙烯氨基甲酸酯和酰胺的环化反应合成2,3-取代吡咯类化合物
Gavin J Rustin,Matthew G Donahue
Gavin J Rustin
A three-step sequence to construct pyrroles from three components including 2,2-dimethoxyethylamine, aryl/alkyl sulfonyl chlorides and alkynes bearing electron-withdrawing groups is presented. The pyrroles are proposed to arise via a 5-exo-...
Stereoselective synthesis of photoactivatable Man(β1,4)GlcNAc-based bioorthogonal probes [0.03%]
用于糖生物学研究的Man(β1,4)GlcNAc衍生物光激活型 bio正交探针的立体选择性合成
Abdullah A Hassan,Mia L Huang
Abdullah A Hassan
We report an operationally facile protocol to prepare photoactivatable probes of the bioactive mammalian disaccharide, Man(β1,4)GlcNAc. Using conformationally restricted mannosyl hemi-acetal donors in a one-pot chlorination, iodination and...
Efficient Syntheses of KLS-13019 Using Palladium Mediated Cross Couplings [0.03%]
钯介导的交叉偶联反应合成KLS-13019的有效方法研究
William A Kinney,Mark E McDonnell,Stanley Freeman et al.
William A Kinney et al.
KLS-13019 is a structural analogue of cannabidiol, that shows improved bioavailability and potency in both preventing and reversing paclitaxel-induced neurotoxicity in vitro and in vivo. KLS-13019 was selected as a development candidate and...
Total Synthesis of (±)- N-Methyldibromoisophakellin and N-Methylugibohlin via Net [3+2] Cycloguanidinylations Employing 2-Amido-1,3-Diamino-Allyl Cations [0.03%]
通过2-酰胺-1,3-二氨基-烯丙基离子进行的[3+2]环瓜尔米丁化实现N-甲基金刚藤碱和N-甲基金刚乌比林的全合成
Nobuyuki Matsumoto,Taehwan Hwang,Daniel Romo
Nobuyuki Matsumoto
A concise total synthesis of (±)-N-methyldibromoisophakellin, a member of the monomeric pyrrole-aminoimidazole alkaloid family isolated from the marine sponge Stylissa carbica, was achieved via a net [3+2] cycloaddition to install the cycl...
One-Pot High-throughput Synthesis of N 3-Substituted 5-Arylidene-2-Thiohydantoin Amides and Acids [0.03%]
一步合成N3取代的5-芳亚甲基-2-硫杂氢定酰胺及酸类化合物的方法及其应用
Chelsi Whitely,Yangmei Li
Chelsi Whitely
A one-pot high-throughput solid-phase method for the synthesis of N3-substituted 5-arylidene-2-thiohydantoin amide and acid has been developed. A tandem ring-closure and ring-open pathway is proposed as the mechanism of forming the two prod...