5503-73-1Relevant academic research and scientific papers
Acyl Radicals from Benzothiazolines: Synthons for Alkylation, Alkenylation, and Alkynylation Reactions
Li, Lei,Guo, Shan,Wang, Qi,Zhu, Jin
supporting information, p. 5462 - 5466 (2019/08/01)
We describe herein a fundamentally new visible light-driven homolytic C-C bond breaking mode for the generation of acyl radicals from C2-acyl-substituted benzothiazolines. The reactive species can be used as versatile synthons for formal radical alkylatio
Benzothiazolines as radical transfer reagents: Hydroalkylation and hydroacylation of alkenes by radical generation under photoirradiation conditions
Uchikura, Tatsuhiro,Moriyama, Kaworuko,Toda, Mitsuhiro,Mouri, Toshiki,Ibá?ez, Ignacio,Akiyama, Takahiko
supporting information, p. 11171 - 11174 (2019/09/30)
Novel radical transfer reagents under photoirradiation conditions were developed by the use of benzothiazoline derivatives. These reagents enabled both hydroalkylation and hydroacylation of alkenes under neutral conditions at ambient temperature without a
Microtubing-Reactor-Assisted Aliphatic C?H Functionalization with HCl as a Hydrogen-Atom-Transfer Catalyst Precursor in Conjunction with an Organic Photoredox Catalyst
Deng, Hong-Ping,Zhou, Quan,Wu, Jie
supporting information, p. 12661 - 12665 (2018/09/20)
Chlorine radical, which is classically generated by the homolysis of Cl2 under UV irradiation, can abstract a hydrogen atom from an unactivated C(sp3)?H bond. We herein demonstrate the use of HCl as an effective hydrogen-atom-transfer catalyst precursor activated by an organic acridinium photoredox catalyst under visible-light irradiation for C?H alkylation and allylation. The key to success relied on the utilization of microtubing reactors to maintain the volatile HCl catalyst. This photomediated chlorine-based C?H activation protocol is effective for a variety of unactivated C(sp3)?H bond patterns, even with primary C(sp3)?H bonds, as in ethane. The merit of this strategy is illustrated by rapid access to several pharmaceutical drugs from abundant unfunctionalized alkane feedstocks.
Corrole-imide dyads - Synthesis and optical properties
Voloshchuk, Roman,Tasior, Mariusz,Ciuciu, Adina I.,Flamigni, Lucia,Gryko, Daniel T.
, p. 479 - 491 (2015/05/05)
Two rarely seen building blocks have been incorporated into light absorbing arrays: corroles and 2,3-naphthalimides. General synthetic strategy consisting in direct condensation of formyl substituted aromatic imides with dipyrranes led to diverse range of
CH-01 is a hypoxia-activated prodrug that sensitizes cells to hypoxia/reoxygenation through inhibition of Chk1 and aurora A
Cazares-Koerner, Cindy,Pires, Isabel M.,Swallow, I. Diane,Grayer, Samuel C.,O'Connor, Liam J.,Olcina, Monica M.,Christlieb, Martin,Conway, Stuart J.,Hammond, Ester M.
, p. 1451 - 1459 (2013/08/23)
The increased resistance of hypoxic cells to all forms of cancer therapy presents a major barrier to the successful treatment of most solid tumors. Inhibition of the essential kinase Checkpoint kinase 1 (Chk1) has been described as a promising cancer therapy for tumors with high levels of hypoxia-induced replication stress. However, as inhibition of Chk1 affects normal replication and induces DNA damage, these agents also have the potential to induce genomic instability and contribute to tumorigenesis. To overcome this problem, we have developed a bioreductive prodrug, which functions as a Chk1/Aurora A inhibitor specifically in hypoxic conditions. To achieve this activity, a key functionality on the Chk1 inhibitor (CH-01) is masked by a bioreductive group, rendering the compound inactive as a Chk1/Aurora A inhibitor. Reduction of the bioreductive group nitro moiety, under hypoxic conditions, reveals an electron-donating substituent that leads to fragmentation of the molecule, affording the active inhibitor. Most importantly, we show a significant loss of viability in cancer cell lines exposed to hypoxia in the presence of CH-01. This novel approach targets the most aggressive and therapy-resistant tumor fraction while protecting normal tissue from therapy-induced genomic instability.
Novel, Cyclically Substituted Furopyrimidine Derivatives and Use Thereof
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Page/Page column 19, (2011/06/19)
The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
A NHC-Involved, cascade, metal-free, and three-component synthesis of 2,3-diarylated fully substituted furans under solvent-free conditions
Yu, Chenxia,Lu, Jun,Li, Tuanjie,Wang, Donglin,Qin, Binbin,Zhang, Honghong,Yao, Changsheng
, p. 2420 - 2424 (2011/11/05)
An efficient synthesis of 2,3-diarylated fully substituted furans was performed through the sequential reactions of Knoevenagel reaction, Stetter reaction catalyzed by NHC, and intramolecular cyclization under solvent-free conditions. The protocol has the
An Efficient synthesis of 2-aminofuran-3-carbonitriles via cascade Stetter-γ-ketonitrile cyclization reaction catalyzed by N-heterocyclic carbene
Liu, Peng,Lei, Min,Ma, Lei,Hu, Lihong
supporting information; experimental part, p. 1133 - 1136 (2011/06/24)
An efficient method for the synthesis of 4,5-disubstituted 2-aminofuran-3-carbonitriles via a cascade Stetter-γ-ketonitrile cyclization reaction of aromatic aldehydes with acylidenemalononitriles, catalyzed by N-heterocyclic carbenes, has been developed.
Fused Bicyclic and Tricyclic Pyrimidine Compounds as Tyrosine Kinase Inhibitors
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Page/Page column 48, (2010/06/11)
Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.
Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor
Coumar, Mohane Selvaraj,Tsai, Ming-Tsung,Chu, Chang-Ying,Uang, Biing-Jiun,Lin, Wen-Hsing,Chang, Chun-Yu,Chang, Teng-Yuan,Leou, Jiun-Shyang,Teng, Chi-Huang,Wu, Jian-Sung,Fang, Ming-Yu,Chen, Chun-Hwa,Hsu, John T.-A.,Wu, Su-Ying,Chao, Yu-Sheng,Hsieh, Hsing-Pang
experimental part, p. 255 - 267 (2010/12/18)
Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocy
