- Mn(III)-mediated phosphinoylation of aldehyde hydrazones: Direct “one-pot” synthesis of α-iminophosphine oxides from aldehydes
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A “one-pot” strategy for the straightforward Mn(III)-mediated phosphinoylation of aldehyde hydrazones with diphenylphosphine oxide to furnish α-iminophosphine oxides is described. This mild and practical method allows the direct use of aldehydes as substrates in one pot to generate the hydrazones, which are then engaged “in situ” by the phosphorus reagent in the presence of Mn(OAc)3 oxidant. Thus, the requisite isolation of the hydrazones is not needed in this operation. Conducted mechanistic experiments implicate a pathway involving phosphorus-centered radicals.
- Bian, Xue-Wei,Zhang, Ling,Shoberu, Adedamola,Zou, Jian-Ping
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supporting information
(2021/04/02)
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- A Green Synthesis and Antibacterial Activity of N-Arylsulfonylhydrazone Compounds
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A green method has been developed for the synthesis of N-arylsulfonylhydrazones via a simple grindstone procedure. By grinding mixtures of benzensulfonyl hydrazides and a series of aryl aldehydes or ketones in the mortar using L-tyrosine as catalyst, 24 N
- Yang, Qian,Hao, Wangwang,He, Yangqing,Zhang, Qian,Yu, Xiaojiao,Hua, Yaobing
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p. 152 - 156
(2020/01/28)
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- Tetrazole-Based Probes for Integrated Phenotypic Screening, Affinity-Based Proteome Profiling, and Sensitive Detection of a Cancer Biomarker
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Target-identification phenotypic screening has been a powerful approach in drug discovery; however, it is hindered by difficulties in identifying the underlying cellular targets. To address this challenge, we have combined phenotypic screening of a fully functionalized small-molecule library with competitive affinity-based proteome profiling to map and functionally characterize the targets of screening hits. Using this approach, we identified ANXA2, PDIA3/4, FLAD1, and NOS2 as primary cellular targets of two bioactive molecules that inhibit cancer cell proliferation. We further demonstrated that a panel of probes can label and/or image annexin A2 (a cancer biomarker) from different cancer cell lines, thus providing opportunities for potential cancer diagnosis and therapy.
- Cheng, Ke,Lee, Jun-Seok,Hao, Piliang,Yao, Shao Q.,Ding, Ke,Li, Zhengqiu
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supporting information
p. 15044 - 15048
(2017/11/20)
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- Developing new chemical tools for DNA methyltransferase 1 (DNMT 1): A small-molecule activity-based probe and novel tetrazole-containing inhibitors
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DNA methylation is an important epigenetic modification catalyzed by DNA methyltransferases (DNMTs). Abnormal expression of endogenous DNMTs in human causes alterations in the genome methylation patterns which subsequently lead to the development of cance
- Zhu, Biwei,Ge, Jingyan,Yao, Shao Q.
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p. 2917 - 2927
(2015/03/30)
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- Base-catalyzed N -N bond cleavage of hydrazones: Synthesis of α-amino ketones
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An efficient Cs2CO3-promoted synthesis of α-amino ketones using hydrazines, aldehydes, and α-haloketones as starting materials through a cascade condensation/nucleophilic substitution/N -N bond cleavage route is developed. The carbonyl group plays a key role in this novel N -N bond cleavage process. Breaking good: A novel method of base-catalyzed N -N bond cleavage of hydrazones has been discovered. A variety of α-amino ketones was synthesized using hydrazines, α-haloketones, and benzaldehyde as starting materials through a cascade condensation/ nucleophilic substitution/N -N bond cleavage sequence.
- Tang, Hai-Tao,Zhou, Yun-Bing,Zhu, Yu,Sun, Hong-Chao,Lin, Min,Zhan, Zhuang-Ping
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supporting information
p. 1278 - 1281
(2014/05/06)
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- Tandem reaction of propargyl alcohol and N-sulfonylhydrazone: Synthesis of dihydropyrazole and its utility in the preparation of 3,3-diarylacrylonitrile
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An efficient and straightforward strategy for the synthesis of 4-methylene-1-(phenylsulfonyl)-4,5-dihydro-1H-pyrazole from propargyl alcohol and N-sulfonylhydrazone is described. N-Sulfonyl allenamide is postulated to be the key intermediate for this tandem transformation.
- Zhu, Yuanxun,Wen, Shan,Yin, Guangwei,Hong, Deng,Lu, Ping,Wang, Yanguang
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supporting information; experimental part
p. 3553 - 3555
(2011/09/14)
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- Synthesis and evaluation of photoreactive tetrazole amino acids
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Image Persented Six photoreactive tetrazole amino acids were efficiently synthesized either by the de novo Kakehi tetrazole synthesis method or by alkylation of a glycine Schiff base with tetrazole-containing alkyl halides, and four of them showed excellent reactivity toward a simple alkene in the photoinduced 1,3-dipolar cycloaddition reaction in acetonitrile/PBS buffer (1:1) mixture.
- Wang, Yizhong,Lin, Qing
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supporting information; experimental part
p. 3570 - 3573
(2011/02/22)
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- Arylsulphonyl hydrazones as blowing agents
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The use of arylsulphonyl hydrazones corresponding to the following general formula: wherein Ar represents a benzene, naphthalene, diphenyl, diphenyl ether, diphenyl sulphone or diphenylene oxide radical which may be substituted by methyl and/or chlorine; R represents the radical of an aldehyde or ketone without the carbonyl oxygen atom; and x represents 1 or 2; as blowing agents for the production of cellular or porous plastics articles.
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