Asymmetric Iodoaminocyclization for the Synthesis of Chiral 2-Heteroaryl Pyrrolidines [0.03%]
用于合成手性2-杂芳基吡咯烷的不对称碘胺环化反应
Yangyang Zhong,Kehan Zhao,Kewen Zhong et al.
Yangyang Zhong et al.
An asymmetric iodoaminocyclization strategy catalyzed by (DHQD)2PHAL has been developed for the synthesis of chiral 2-heteroaryl pyrrolidines, including 2-purinyl and 2-indolyl analogues. This method proceeds under mild conditions and affor...
A Palladium(II)-Catalyzed Dehydrogenative Strategy to NIR-Emissive BODIPY Dimers and Trimers with Reactive Oxygen Species Generation Characteristics [0.03%]
一种 palladium(II) 催化的 NIR 发光 BODIPY 二聚体和三聚体的脱氢构筑策略并具有产生活性氧的特点
Chunyan Pan,Zhengxin Kang,Fan Lv et al.
Chunyan Pan et al.
A highly regioselective, one-pot synthesis of directly β,β-linked BODIPY dimers and trimers via a novel palladium-catalyzed oxidative C-H coupling is reported. These oligomers exhibit intense intramolecular J-type exciton coupling, leadin...
Chiral Phosphoric Acid-Catalyzed Asymmetric [4 + 2] Cycloadditions of Photogenerated o-Quinodimethanes with Vinylazaarenes [0.03%]
手性磷酸催化o-醌二甲烷与 vinylazaarenes的光激发[4+2]环加成反应及不对称合成
Shu-Wei Gan,Yu Zhou,Yu-Mei Ma et al.
Shu-Wei Gan et al.
Chiral cyclohexyl-appended azaarenes are highly sought synthetic targets in biochemistry and medicinal chemistry. Herein we report a chiral phosphoric acid-catalyzed asymmetric [4 + 2] cycloaddition reaction between photogenerated o-quinodi...
Electrochemical Cascade Reaction for C(sp3)-H Tetrazolation of Saturated Heterocycles: Access to Tetrazole-5-thiones [0.03%]
饱和杂环C(sp3)-H四氮唑化反应合成四氮唑-5-硫酮类化合物的新方法
Xiao Yu,Xian Liu,Shengkui Jin et al.
Xiao Yu et al.
Tetrazole-5-thiones, known for their biological activities, are synthesized electrochemically through a cascade reaction using commercially available isothiocyanates, azidotrimethylsilane, and heterocycles. This method not only broadens the...
Seeking Equality from an Asymmetric System: The Convergent Total Synthesis of Prostacyclin Drug (±)-Beraprost Sodium [0.03%]
从不对称系统中寻求对等性：前列环素药物（±）-贝前列素钠的汇聚式全合成
Xinyu Zhu,Zhihao Qi,Jingfan Pan et al.
Xinyu Zhu et al.
(±)-Beraprost sodium is an oral prostacyclin drug used to treat pulmonary arterial hypertension (PAH). It exists as a mixture of two C-4 diastereomers in a ratio of approximately 1:1, which presents significant challenges for process devel...
Direct Synthesis of Tricyclo[3.2.1.02,7]octenes via Palladium-Catalyzed Sequential Reactions of 2-Pyranones with 1,3-Dienes [0.03%]
通过钯催化2-吡喃酮与1,3-丁二烯的连续反应直接合成三环[3.2.1.02,7]辛烯化合物
Jian-Bang Hu,Xin-Lian Liu,Wen-Hua Gao et al.
Jian-Bang Hu et al.
Given the widespread use of tricyclo[3.2.1.02,7]octene scaffolds in natural medicinal chemistry and biology, the development of methods for their synthesis remains important. Here, a palladium-catalyzed sequential [4 + 2]-cycloaddition/deca...
N-Alkylsulfonamide Nucleophilicity: Experimental and Computational Assessment of Nitrogen Nucleophilicity of (S)-2-(Iodomethyl)-1-tosylpyrrolidine [0.03%]
氮亲核性：(S)-2-（碘甲基）-1-对甲苯磺酰基吡咯烷氮亲核性的实验和计算评估
Julien Escudero,Tomohiro Yasukawa,Pengchen Ma et al.
Julien Escudero et al.
Sulfonamides are generally considered to be non-nucleophilic due to the presence of a sulfonyl group. We show that N-alkylsulfonamides are sufficiently basic/nucleophilic to be protonated and react with electrophilic centers. Contrasts with...
Synthesis of 1,3-Bis-trifluoromethylated (Hetero)cyclohexane-2-carboxylates from Alkylidenemalononitriles [0.03%]
由烯基甲基酮腈合成1,3-双三氟甲基化环己烷-2-羧酸酯类化合物
Morgane Mando,Akash R Gogate,Dylan J Smith et al.
Morgane Mando et al.
Reported herein is a method for the syn-selective 1,3-bis-trifluoromethylation of (hetero)cycloalkylidenemalononitriles. The malononitrile-containing intermediate can be readily converted into carboxylates (and derivatives thereof) by oxida...
Solution-Phase and Mechanochemical Brønsted-Acid-Catalyzed N-Alkylation of NH-Heterocycles via Hydroamination of Vinyl Ethers [0.03%]
通过乙烯基醚的氢胺化有效进行杂环化合物N-烷基化的溶液和机械化学方法
Vikash Kumar,Rajaram Maayuri,L N S Laya Pagadala et al.
Vikash Kumar et al.
A Brønsted-acid-catalyzed hydroamination of vinyl ethers with carbazoles was developed using diphenyl hydrogen phosphate (DPHP) as the catalyst. The method enables the efficient, regioselective N-alkylation of various carbazoles and NH-het...
Nickel-Catalyzed Enantioselective Reductive Alkenylation of N-Pyridyl Aldimines via a Mechanism of Elementary 1,4-Addition [0.03%]
镍催化N-吡啶亚胺的对映选择性还原烯基化反应的新机理研究
Mengxin Zhao,Bo Xiao,Lantian Sun et al.
Mengxin Zhao et al.
Chiral nickel complexes of isoquinox catalyze an asymmetric reductive alkenylation of N-picolyl aldimines with readily available alkenyl bromides, triflates, and tosylates as carbon electrophiles. The method features neutral and mild condit...