1530-88-7Relevant academic research and scientific papers
Isoform-selective substrates of nitric oxide synthase
Jia, Qiang,Cai, Tingwei,Huang, Mingchuan,Li, Huiying,Xian, Ming,Poulos, Thomas L.,Wang, Peng G.
, p. 2271 - 2274 (2003)
Because of the double-edged nature of NO, the development of isoform-selective NOS substrates is a highly desirable goal. Given the striking similarity in the heme active sites of the three NOS isoforms, it presents an challenging problem. Several N-aryl-N′-hydroxyguanidines have recently been shown as substrates that are selective for iNOS over nNOS. Here, we report the first success that 3 is a good substrate for nNOS (70% activity of NOHA, Km ≈ 40 ± 6 μM) over iNOS.
N-Cyanation of Primary and Secondary Amines with Cyanobenzio-doxolone (CBX) Reagent
Chen, Zimin,Yuan, Weiming
supporting information, p. 14836 - 14840 (2021/09/30)
An efficient electrophilic N-cyanation of amines with a stable and less-toxic cyanobenziodoxole reagent towards the synthesis of cyanamides is disclosed. This synthetically practicable strategy allows the construction of a wide variety of cyanamides under very mild and simple conditions with a broad functional group compatibility, and showcases a huge potential in late-stage modification of complex molecules.
Synthesis method of cyanamide
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Paragraph 0047-0048, (2021/08/06)
The invention relates to the field of synthesis of chemical products, in particular to a synthesis method of a cyanamide compound. According to the method, cyanamide is efficiently synthesized under the conditions of air and room temperature by starting from easily available secondary amine compounds, taking cheap and green TMSCN as a cyanide source and adopting green and pollution-free current as a reaction driving agent. Compared with a conventional cyanamide synthesis method, the method disclosed by the invention has the obvious advantages of cheap and easily available reaction raw materials, minimum environmental pollution caused by current, good tolerance to various functional groups on aromatic rings and alicyclic rings, high yield and the like. The method disclosed by the invention can be widely applied to synthesis in the fields of medicines, materials, natural products and the like in industrial and academic circles.
Electrochemical strategies for: N -cyanation of secondary amines and α C -cyanation of tertiary amines under transition metal-free conditions
Cai, Hu,Fu, Yaping,Fu, Zhengjiang,Guo, Shengmei,Hao, Guangguo,Yi, Xuezheng,Yin, Jian,Zhong, Tingting
supporting information, p. 9422 - 9427 (2021/12/09)
Transition metal-free electrochemical approaches for the N-cyanation of secondary amines and the α C-cyanation of tertiary amines have been well established, with products being obtained in moderate to good yields and with good functional group tolerance under ambient conditions. The synthetic application of the protocols has been highlighted through scale-up experiments in a galvanostatic mode. Preliminary mechanistic investigation has confirmed that TBAB played a critical role in N-cyanation transformation and has indicated that the transformation might proceed via a free radical process. This journal is
Tris(3,5-dimethylpyrazolyl)methane copper(I) complexes featuring one disubstituted cyanamide ligand
Melekhova, Anna A.,Novikov, Alexander S.,Dubovtsev, Alexey Yu.,Zolotarev, Andrey A.,Bokach, Nadezhda A.
, p. 69 - 74 (2018/09/22)
The complexes [Cu{HC(3,5-Me2pz)3}(NCNR2)][BF4] (1–8; R2 = Me2 1, Et2 2, C5H10 3, C4H8O 4, C4H8 5, C3H
A allyl uncle amine compound by one-step synthesis method of cyano uncle amine compound (by machine translation)
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Paragraph 0034-0042, (2017/09/01)
The invention relates to a one-step synthesis of amine compound allyl unclecyano uncle amine compounds, which belongs to the technical field of organic synthetic method. The method specific synthetic process is as follows: in the airtight reaction environment, to the anhydrous organic solvent is added in the cyanogen bromide, under protection of inert gas, and then added dropwise to the solution in the allylic and high yield amine compound, to obtain allyl uncle amine compound concentration is 0.8 - 1 mol/L solution, at room temperature the reaction 16 - 24 hours later, after column chromatography separation and purification, to obtain a corresponding cyano uncle amine compound. The method to get rid of the expensive deallylation use of the catalyst, the synthesis step is less, raw materials are easy, cheap, mild reaction conditions, the operation is simple, easy to craft and industrialization. Yield 50% - 80% between. (by machine translation)
Synthesis of Cyanamides from Cyanogen Bromide under Mild Conditions through N-Cyanation of Allylic Tertiary Amines
Liang, Honggang,Bao, Lingxiang,Du, Yao,Zhang, Yiying,Pang, Siping,Sun, Chenghui
supporting information, p. 2675 - 2679 (2017/10/06)
Cyanamides were selectively formed through a one-step nucleophilic substitution reaction of allylic tertiary amines with cyanogen bromide. Because of the mild reaction conditions and good yields of the reaction, as well as the commercial availability of the starting materials, this new method represents a valuable tool for the synthesis of cyan-amides through an N-deallylation reaction and an N-cyanation reaction in one pot.
N-Cyanation of Secondary Amines Using Trichloroacetonitrile
Ayres, James N.,Ling, Kenneth B.,Morrill, Louis C.
supporting information, p. 5528 - 5531 (2016/11/17)
A one-pot N-cyanation of secondary amines has been developed using trichloroacetonitrile as an inexpensive cyano source. A diverse range of cyclic and acyclic secondary amines can be readily transformed into the corresponding cyanamides in good isolated yields, with the method successfully utilized in the final synthetic step of a biologically active rolipram-derived cyanamide. This approach exhibits distinct selectivity when compared to the use of highly toxic cyanogen bromide.
3,5-Disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof
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, (2008/06/13)
Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D are defined herein. The present invention relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
