904078-20-2Relevant academic research and scientific papers
Anti-oligomerization sheet molecules: Design, synthesis and evaluation of inhibitory activities against α-synuclein aggregation
Liu, Hao,Chen, Li,Zhou, Fei,Zhang, Yun-Xiao,Xu, Ji,Xu, Meng,Bai, Su-Ping
supporting information, p. 3089 - 3096 (2019/06/14)
Aggregation of α-synuclein (α-Syn) play a key role in the development of Parkinson Disease (PD). One of the effective approaches is to stabilize the native, monomeric protein with suitable molecule ligands. We have designed and synthesized a series of sheet-like conjugated compounds which possess different skeletons and various heteroatoms in the two blocks located at both ends of linker, which have good π-electron delocalization and high ability of hydrogen-bond formation. They have shown anti-aggregation activities in vitro towards α-Syn with IC50 down to 1.09 μM. The molecule is found binding in parallel to the NACore within NAC domain of α-Syn, interfering aggregation of NAC region within different α-Syn monomer, and further inhibiting or slowing down the formation of α-Syn oligomer nuclei at lag phase. The potential inhibitor obtained by our strategy is considered to be highly efficient to inhibit α-Syn aggregation.
A One-Pot, fast, and efficient amidation of carboxylic acids, α-amino acids and sulfonic acids using pph3/n-chlorobenzotriazole system
Rouhi-Saadabad, Hamed,Akhlaghinia, Batool
, p. 1703 - 1714 (2015/09/15)
Triphenylphosphine (PPh3)/N-chlorobenzotriazole (NCBT), and amine (primary and secondary aliphatic amines and also substituted anilines) in CH2Cl2 efficiently converted carboxylic acids, α-amino acids, and sulfonic acids to the corresponding amides and sulfonamides at room temperature. Good to excellent yields, inexpensive, and fast reaction conditions are the important features of this procedure.
Phosphine-based redox catalysis in the direct traceless staudinger ligation of carboxylic acids and azides
Kosal, Andrew D.,Wilson, Erin E.,Ashfeld, Brandon L.
supporting information, p. 12036 - 12040 (2013/01/16)
Redox catalysis: Aryl amides, imides, lactams, and dipeptides are obtained through a direct Staudinger ligation mediated by phosphine-based redox catalysis (see scheme). Mechanistic studies indicate the involvement of a phosphonium carboxylate intermediate that leads to a 1,3-acyl migration and thus results in C-N bond formation. Copyright
Mo(CO)6-mediated carbamoylation of aryl halides
Ren, Wei,Yamane, Motoki
experimental part, p. 8410 - 8415 (2011/02/23)
A simple method for the synthesis of amides has been developed by molybdenum-mediated carbamoylation of aryl halides. Whereas the conventional palladium-catalyzed three-component coupling reaction requires a large excess of gaseous carbon monoxide, the incorporation of carbon monoxide in this Mo-mediated carbamoylation reaction is so efficient that it requires only a slight excess amount of carbon monoxide in the form of its molybdenum complex, Mo(CO)6. The reaction is applicable for the synthesis of a wide variety of not only secondary and tertiary amides but also primary amides by using aqueous ammonia.
Carbamoylation of aryl halides by molybdenum or tungsten carbonyl amine complexes
Ren, Wei,Yamane, Motoki
supporting information; experimental part, p. 3017 - 3020 (2010/07/05)
When aryl halide is treated with molybdenum carbonyl amine complex in the presence of base, carbamoylation proceeds to give amide in good yield. The proposed mechanism involves oxidative addition of aryl halide to molybdenum(0) complex, migratory insertio
Palladium-catalyzed carbamoylation of aryl halides by tungsten carbonyl amine complex
Wei, Ren,Yamane, Motoki
supporting information; experimental part, p. 8332 - 8335 (2010/02/17)
(Chemical Equation Presented) In the presence of aminepentacarbonyltungsten, base, and a catalytic amount of palladium(0) complex, carbamoylation of aryl halide proceeds to afford amide. The reaction may involve transmetalation between palladium(II) inter
