1519044-12-2Relevant academic research and scientific papers
Method for preparing 2-iodo aryl ether under action of alkali metal hydride
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Page/Page column 8, (2021/06/22)
The invention discloses a method for preparing 2-iodo aryl ether under the action of alkali metal hydride, which comprises the following steps: adding alkali metal hydride and phenol into a solvent, then adding 1, 2-diiodo aromatic hydrocarbon, and reacti
COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME
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Paragraph 0080-0082, (2019/04/14)
Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): wherein Y is an oxygen atom or a sulfur atom; X1 and X2 are each independently C(Ra), the two (Ra)s are the same or different, and the two (Ra)s are joined together to form a first aryl ring; X3 and X4 are each independently C(Rb), the two (Rb)s are the same or different, and the two (Rb)s are joined to form a second aryl ring or a heteroaryl ring.
COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME
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Paragraph 0087; 0093-0095, (2018/06/15)
Provided are a novel compound and an organic electronic device using the same. The novel corn pound is represented by the following Formula (I): wherein Y is an oxygen atom, a sulfur atom, or a sulfur dioxide group; X1 and X2 are each independently C(Ra), multiple (Ra)s are the same or different, and the two (Ra)s are joined together to form a first aryl ring; X3 and X4 are each independently C(Rb), multiple (Rb)s are the same or different, and the two (Rb)s are joined to form a second aryl ring or a heteroaryl ring.
COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME
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Paragraph 0061; 0062; 0067; 0068, (2019/04/30)
Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): wherein Y is an oxygen atom or a sulfur atom; X 1and X 2are each independently C(R a), the two(R a)s are the same or different, and the two (R a)s are joined together to form a first aryl ring; X 3and X 4are each independently C(R b), the two (R b)s are the same or different, and the two (R b)s are joined to form a second aryl ring or a heteroaryl ring.
Synthesis of medium-sized (6-7-6) ring compounds by iron-catalyzed dehydrogenative C-H activation/annulation
Panda, Niranjan,Mattan, Irshad,Ojha, Subhadra,Purohit, Chandra Shekhar
, p. 7861 - 7870 (2018/11/21)
In this report, we have described a FeCl3-catalyzed process involving intramolecular annulation of o-phenoxy diarylacetylenes via hydroarylation to afford a series of biologically potent fused seven-membered (6-7-6) ring compounds under mild reaction conditions. This reaction was believed to proceed through Friedel-Crafts type sequential carbometallation followed by protonation to produce phenyldibenz[b,f]oxepines. This method was also extended to synthesize seven-membered rings that are fused with coumarins.
Intramolecular Aryl Migration of Diaryliodonium Salts: Access to ortho-Iodo Diaryl Ethers
Chen, Huangguan,Han, Jianwei,Wang, Limin
supporting information, p. 12313 - 12317 (2018/09/10)
By using vicinal trifluoromethanesulfonate-substituted diaryliodonium salts, a novel approach was developed for the synthesis of ortho-iodo diaryl ethers by intramolecular aryl migration. The reaction conditions are mild with a broad substrate scope. Mechanistic insight suggests a sulfonyl-directed nucleophilic aromatic substitution pathway. Additionally, the product ortho-iodo diaryl ethers serve as versatile synthons as demonstrated with several coupling reactions. Furthermore, a useful thyroxine analogue of the 3-iodo-l-thyronine (3-T1) derivative was synthesized by this aryl migration procedure.
Development of 3-phenyl-N-(2-(3-phenylureido)ethyl)-thiophene-2-sulfonamide compounds as inhibitors of antiapoptotic Bcl-2 family proteins
Yang, Chengwen,Chen, Sha,Zhou, Mi,Li, Yan,Li, Yangfeng,Zhang, Zhengxi,Liu, Zhen,Ba, Qian,Li, Jingquan,Wang, Hui,Yan, Xiaomei,Ma, Dawei,Wang, Renxiao
supporting information, p. 1436 - 1452 (2014/07/21)
Antiapoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2, and Mcl-1, are often overexpressed in tumor cells, which contributes to tumor cell resistance to chemotherapies and radiotherapies. Inhibitors of these proteins thus have potential applications in cancer treatment. We discovered, through structure-based virtual screening, a lead compound with micromolar binding affinity to Mcl-1 (inhibition constant (Ki)=3 μM). It contains a phenyltetrazole and a hydrazinecarbothioamide moiety, and it represents a structural scaffold not observed among known Bcl-2 inhibitors. This work presents the structural optimization of this lead compound. By following the scaffold-hopping strategy, we have designed and synthesized a total of 82 compounds in three sets. All of the compounds were evaluated in a fluorescence-polarization binding assay to measure their binding affinities to Bcl-xL, Bcl-2, and Mcl-1. Some of the compounds with a 3-phenylthiophene-2-sulfonamide core moiety showed sub-micromolar binding affinities to Mcl-1 (Ki=0.3-0.4 μM) or Bcl-2 (Ki≈1 μM). They also showed obvious cytotoxicity on tumor cells (IC 50L in a similar mode to ABT-737. Several apoptotic assays conducted on HL-60 cells demonstrated that these compounds are able to induce cell apoptosis through the mitochondrial pathway. We propose that the compounds with the 3-phenylthiophene-2-sulfonamide core moiety are worth further optimization as effective apoptosis inducers with an interesting selectivity towards Mcl-1 and Bcl-2. Hopping to inhibition: Several sets of derivatives of a lead compound have been designed and synthesized by following the scaffold-hopping strategy, and active compounds containing a 3-phenylthiophene-2-sulfonamide core moiety have been obtained. The most potent compounds have sub-micromolar binding affinity to the antiapoptotic protein Mcl-1 and are effective apoptosis inducers in living cells.
