63991-67-3Relevant academic research and scientific papers
Hydrosilylative reduction of primary amides to primary amines catalyzed by a terminal [Ni-OH] complex
Pandey, Pragati,Bera, Jitendra K.
supporting information, p. 9204 - 9207 (2021/09/20)
A terminal [Ni-OH] complex1, supported by triflamide-functionalized NHC ligands, catalyzes the hydrosilylative reduction of a range of primary amides into primary amines in good to excellent yields under base-free conditions with key functional group tolerance. Catalyst1is also effective for the reduction of a variety of tertiary and secondary amides. In contrast to literature reports, the reactivity of1towards amide reduction follows an inverse trend,i.e., 1° amide > 3° amide > 2° amide. The reaction does not follow a usual dehydration pathway.
Catalytic N-Acylation of Cyclic Amines by Arylglyoxylic Acids via Radical-Radical Cross-Coupling
Bhadra, Sukalyan,Gupta, Aniket,Kumar Singh, Anupam,Rahaman, Ajijur
supporting information, p. 2198 - 2202 (2021/07/22)
A methodical mechanistic investigation allowed for the catalytic N-acylation of secondary cyclic amine counterparts by arylglyoxylic acids through radical-radical coupling. The reaction proceeds via a twofold SET-promoted Cu(I)/Cu(II) catalytic cycle under mild conditions. An analogous reaction variant allows for the N-acylation in a one-pot fashion directly starting from a secondary cyclic amine even in the presence of a second amine or hydroxy group.
GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington's Disease-Related Phenotypes
Wang, Congcong,Zhang, Yu-Fang,Guo, Shimeng,Zhao, Quan,Zeng, Yanping,Xie, Zhicheng,Xie, Xin,Lu, Boxun,Hu, Youhong
, p. 941 - 957 (2020/11/30)
GPR52 is an orphan G protein-coupled receptor (GPCR) that has been recently implicated as a potential drug target of Huntington's disease (HD), an incurable monogenic neurodegenerative disorder. In this research, we found that striatal knockdown of GPR52 reduces mHTT levels in adult HdhQ140 mice, validating GPR52 as an HD target. In addition, we discovered a highly potent and specific GPR52 antagonist Comp-43 with an IC50 value of 0.63 μM by a structure-activity relationship (SAR) study. Further studies showed that Comp-43 reduces mHTT levels by targeting GPR52 and promotes survival of mouse primary striatal neurons. Moreover, in vivo study showed that Comp-43 not only reduces mHTT levels but also rescues HD-related phenotypes in HdhQ140 mice. Taken together, our study confirms that inhibition of GPR52 is a promising strategy for HD therapy, and the GPR52 antagonist Comp-43 might serve as a lead compound for further investigation.
A piperazine amide preparation method of the compound (by machine translation)
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Paragraph 0037-0039, (2017/08/25)
The invention discloses a piperazine amides preparation method, comprising: in a solvent, the compound 1 with compound 2 to carry out the reaction, to obtain compound 3, the reaction temperature is 20 °C -120 °C; Ar is substituted or unsubstituted aryl; R is hydrogen, methyl, ethyl, propyl, benzyl, tert-butoxy carbonyl, benzyloxycarbonyl, C1 - C3 Acyl, or substituted or unsubstituted aryl; the aromatic vuill substituted ethylenically C1 - C5 Straight or branched chain alkyl, C1 - C3 Alkoxy, amino, halogen, cyano, aldehyde, C1 - C5 Acyl, trifluoromethyl and carboxyl in the one or more; the aromatic substituent is phenyl, thienyl, pyrrolyl, pyrimidinyl or pyridinyl. Preparation method of this invention mild condition, raw material properties are stable, easy to use and storage, high yield, the process is simple, low requirements on equipment, after treatment is convenient, product separation and purification is simple. (by machine translation)
Mesoporous niobium oxide spheres as an effective catalyst for the transamidation of primary amides with amines
Ghosh, Subhash Chandra,Li, Cheng Chao,Zeng, Hua Chun,Ngiam, Joyce S. Y.,Seayad, Abdul M.,Chen, Anqi
, p. 475 - 484 (2014/05/20)
Mesoporous niobium oxide spheres (MNOS), conveniently prepared by a novel antisolvent precipitation approach, have been shown to be an effective catalyst for the transamidation of primary amides with amines. This novel transamidation can be efficiently carried out under solvent-free conditions and is applicable to a wide range of primary amides and amines to provide N-alkyl amides in good to excellent yields. The catalyst is highly stable and reusable. The application of this transamidation reaction has been demonstrated in the synthesis of antidepressant drug moclobemide and other druglike compounds.
Aerobic oxidative amidation of aromatic and cinnamic aldehydes with secondary amines by CuI/2-pyridonate catalytic system
Zhu, Mingwen,Fujita, Ken-Ichi,Yamaguchi, Ryohei
, p. 9102 - 9109,8 (2012/12/11)
A simple and convenient CuI/2-pyridonate catalytic system for the oxidative amidation of aldehydes with secondary amines has been developed. With this system, a variety of useful arylamides have been synthesized in moderate to good yields in the presence of small amount of copper catalyst and the pyridonate ligand, generating only water as a coproduct. Synthesis of cinnamamides was also achieved by the reactions of cinnamaldehydes with secondary amines in moderate yields. Air was successfully employed as a green oxidant in this catalytic system, achieving a safe and atom-efficient system for the synthesis of amides.
Direct reductive amination of carbonyl compounds using bis(triphenylphosphine) copper(I) tetrahydroborate
Bhanushali, Mayur J.,Nandurkar, Nitin S.,Bhor, Malhari D.,Bhanage, Bhalchandra M.
, p. 1273 - 1276 (2007/10/03)
A direct reductive amination protocol for aldehydes/ketones using bis(triphenylphosphine) copper(I) tetrahydroborate as a novel reducing agent in the presence of sulfamic acid has been developed. The reagent chemoselectively reduces the imine moiety and does not affect other reducible functionalities such as chloro, nitro, cyano and methoxy.
Fused imidazopyridine derivatives as antihyperlipidemic agents
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, (2008/06/13)
A novel compound of the formula: wherein ring Q is an optionally substituted pyridine ring; One of R0, R1and R2is —Y0—Z0, and the other tow groups are a hydrogen, a halogen, an optionally substituted hydroxy group, a hydrocarbon group that may be an optionally substituted hydrocarbon group or an acyl group; Y0is a bond or an optionally substituted bivalent hydrocarbon group; Z0is a basic group which may be bonded via oxygen, nitrogen, —CO—, —CS—, —SO2N(R3)— (where R3is hydrogen or an optionally substituted hydrocarbon group), or S(O)n(wherein n is to 0, 1 or 2); .........is a single bond or a double bond, or a salt thereof, which has an excellent LDL receptor up-regulating, blood-lipids lowering, blood-sugar lowering and diabetic complication-ameliorating activity.
Microwave-assisted solvent-free parallel synthesis of thioamides
Olsson,Hansen,Andersson
, p. 7947 - 7950 (2007/10/03)
Rapid parallel synthesis of thioamides is described. A library of amides, synthesised by mixing acyl chlorides and diamines, was transformed into the corresponding thioamides utilising Lawesson's reagent as the oxygen/sulphur exchange reagent. Purification by solid-phase extraction afforded the library members in adequate purities and yields. (C) 2000 Elsevier Science Ltd.
A Novel Cleavage Technique to Generate Small Molecule Compounds and Libraries via a Two-Resin System
Ouyang, Xiaohu,Armstrong, Robert W.,Murphy, Martin M.
, p. 1027 - 1032 (2007/10/03)
Application of organic synthesis to solid supports has led to the successful implementation of combinatorial chemistry in the drug discovery process. This paper describes a novel use of the Hofmann elimination of tetrasubstituted amine salts on solid-phas
