874296-78-3Relevant academic research and scientific papers
TBAI-mediated regioselective sulfenylation of indoles with sulfonyl chlorides in one pot
He, Yongzhao,Jiang, Jun,Bao, Wenhu,Deng, Wei,Xiang, Jiannan
, p. 4583 - 4586 (2017)
A versatile method for the synthesis of 3-sulfenylated indoles via TBAI promoted sulfenylation of indoles with sulfonyl chlorides in one pot has been presented. This system features highly regioselective, metal-free, easy operation, and shows a broad functional group tolerance leading to excellent yields. And this reaction could be easily conducted in 10 mmol scale with high effectivity. A plausible mechanism is proposed.
Iodine/Manganese Catalyzed Sulfenylation of Indole via Dehydrogenative Oxidative Coupling in Anisole
Li, Weihe,Wang, Hao,Liu, Shengping,Feng, Hua,Benassi, Enrico,Qian, Bo
, p. 2666 - 2671 (2020/05/25)
This protocol describes an iodine/manganese catalytic system for dehydrogenative oxidative coupling reaction of indoles with thiols in anisole. Particularly, the dual roles of anisole have been first demonstrated as a solvent and as a promoter via the formation of an oxonium ion intermediate to accelerate the generation of products. A series of sulfenylindoles are readily constructed under aerobic mild reaction conditions. In addition, the achievement for preparing anticancer and anti-AIDS drugs testifies the practicability of this approach. The mechanism studies disclose probable alternative pathways and a single-electron transfer process are involved in this transformation. (Figure presented.).
Nitrosonium ion catalysis: aerobic, metal-free cross-dehydrogenative carbon-heteroatom bond formation
Bering, Luis,D'Ottavio, Laura,Sirvinskaite, Giedre,Antonchick, Andrey P.
supporting information, p. 13022 - 13025 (2018/11/23)
Catalytic cross-dehydrogenative coupling of heteroarenes with thiophenols and phenothiazines has been developed under mild and environmentally benign reaction conditions. For the first time, NOx+ was applied for catalytic C-S and C-N bond formation. A comprehensive scope for the C-H/S-H and C-H/N-H cross-dehydrogenative coupling was demonstrated with >60 examples. The sustainable cross-coupling conditions utilize ambient oxygen as the terminal oxidant, while water is the sole by-product.
Palladium-Catalyzed Oxidative Sulfenylation of Indoles and Related Electron-Rich Heteroarenes with Aryl Boronic Acids and Elemental Sulfur
Li, Jianxiao,Li, Chunsheng,Yang, Shaorong,An, Yanni,Wu, Wanqing,Jiang, Huanfeng
, p. 7771 - 7783 (2016/09/12)
An efficient and convenient palladium-catalyzed C-H bond oxidative sulfenylation of indoles and related electron-rich heteroarenes with aryl boronic acids and elemental sulfur has been described. This procedure provides a useful and direct approach for the assembly of a wide range of structurally diverse 3-sulfenylheteroarenes with moderate to excellent yields from simple and readily available starting materials. Moreover, this synthetic protocol is suitable for N-protected and unprotected indoles. Notably, the construction of two C-S bonds in one step was also achieved in this transformation.
2-(1H-INDOLYLSULFANYL) -ARYL AMINE DERIVATIVES FOR USE IN THE TREATMENT OF AFFECTIVE DISORDERS, PAIN, ADHD AND STRESS URINARY INCONTINENCE
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Page/Page column 40-41, (2008/06/13)
The present invention relates to aniline derivatives of the general formula I as the free base or salts thereof and their use.
