6935-44-0Relevant academic research and scientific papers
Ammonium chloride catalyzed Knoevenagel condensation in PEG-400 as ecofriendly solvent
Waghmare, Smita R.
, p. 849 - 855 (2021/09/28)
A simple and selective green methodology has been successfully developed for Knoevenagel condensation in polyethylene glycol-400 using 10 mol % ammonium chloride as catalyst. The method is applicable to a wide range of aromatic, heteroaromatic and α,β-unsaturated aldehydes. The reactions have been found to be clean and free from the formation of the Michael adduct.
Development of Novel Mitochondrial Pyruvate Carrier Inhibitors to Treat Hair Loss
Liu, Xiaoguang,Flores, Aimee A.,Situ, Lisa,Gu, Wen,Ding, Hui,Christofk, Heather R.,Lowry, William E.,Jung, Michael E.
, p. 2046 - 2063 (2021/02/16)
Herein, we report the synthesis and evaluation of novel analogues of UK-5099 both in vitro and in vivo for the development of mitochondrial pyruvate carrier (MPC) inhibitors to treat hair loss. A comprehensive understanding of the structure-activity relationship was obtained by varying four positions of the hit compound, namely, the alkyl group on the N1 position, substituents on the indole core, various aromatic and heteroaromatic core structures, and various Michael acceptors. The major discovery was that the inhibitors with a 3,5-bis(trifluoromethyl)benzyl group at the N1 position were shown to have much better activity than JXL001 (UK-5099) to increase cellular lactate production. Additionally, analogue JXL069, possessing a 7-azaindole heterocycle, was also shown to have significant MPC inhibition activity, which further increases the chemical space for drug design. Finally, more than 10 analogues were tested on shaved mice by topical treatment and promoted obvious hair growth on mice.
A reusable efficient green catalyst of 2d cu-mof for the click and knoevenagel reaction
Maity, Himadri Sekhar,Maity, Suvendu,Naskar, Kaushik,Sinha, Chittaranjan
, (2021/09/07)
[Cu(CPA)(BDC)]n (CPA = 4-(Chloro-phenyl)-pyridin-4-ylmethylene-amine; BDC = 1,4-benzenedicarboxylate) has been synthesized and structurally characterized by single crystal X-Ray diffraction measurement. The structural studies establish the copper (II) containing 2D sheet with (4,4) square grid structure. The square grid lengths are 10.775 and 10.769 ?. Thermal stability is assessed by TGA, and subsequent PXRD data establish the crystallinity. The surface morphology is evaluated by FE-SEM. The N2 adsorption?desorption analysis demonstrates the mesoporous feature (～6.95 nm) of the Cu-MOF. This porous grid serves as heterogeneous green catalyst with superficial recyclability and thermal stability and facilitates organic transformations efficiently such as, Click and Knoevenagel reactions in the aqueous methanolic medium.
Design, Synthesis, Cytotoxic Screening and Molecular Docking Studies of Novel Hybrid Thiosemicarbazone Derivatives as Anticancer Agents
Mohammed, Faten Zahran,Rizzk, Youstina William,El Deen, Ibrahim Mohey,Mourad, Ahmed A. E.,El Behery, Mohammed
, (2021/11/30)
Thiosemicarbazones have been the focus of scientists owing to their broad clinical anticancer range. Herein, A Series of new thiosemicarbazone derivatives 5–9 were synthesized and confirmed through the use of different spectroscopic techniques along with
One-pot synthesis of nitrogen-doped highly ordered mesoporous polymer nanospheres as a highly efficient catalyst for the water-medium Knoevenagel reactions
Li, Peng,Lv, Fujian,Tan, Xuan,Zhao, Pusu,Zhu, Fengxia
, (2021/11/23)
Nitrogen-doped mesoporous polymer nanospheres (3HP-MPS) with short channel structures were prepared by a template strategy using 3-hydroxypyridine as a nitrogen source. The nitrogen basic active sites are incorporated into the framework of mesoporous poly
Bismuth (III) Triflate: A Mild, Efficient Promoter for the Synthesis of Trisubstituted Alkenes through Knoevenagel Condensation
Datta, Arup
, p. 843 - 849 (2020/11/25)
In this work, smooth efficient and eco-friendly two component coupling method is reported for the synthesis of Knoevenagel Condensation product in presence of Bi(OTf)3 catalyst under solvent free condition. Catalyst has participated in condensation between substituted aldehydes (aromatic and hetero-aromatic) and active methylene compounds (ethyl cyanoacetate, malononitrile and cyanoacetamide) effectively to generate an excellent yield of the product. Bi(OTf)3 catalyst is stable, inexpensive and easily available was used for four times in this reaction without loss of catalytic activity. [Formula Presented]
Water mediated procedure for preparation of stereoselective oximes as inhibitors of MRCK kinase
Luqman, Suaib,Misra, Krishna,Pandey, Jyoti,Shrivash, Manoj Kumar,Shukla, Akhilesh Kumar,Singh, Shilipi
, (2020/07/08)
Stereoselective aldoximes, preferably Z form have been obtained from α-cyano substituted carbonyl conjugated alkenes. This reaction occurs through Michael addition type reaction followed by retro-Knoevenagel reaction without transition-metal catalysis via C–C bond cleavage. These oximes are evaluated against cancer cell lines employing mechanistic study. Two oximes showed significant cytotoxic activity, which through in silico studies were found to inhibit MRCK Kinase, responsible for metastatic spread of cancer mortality.
A facile microwave-assisted Knoevenagel condensation of various aldehydes and ketones using amine-functionalized metal organic frameworks
Lee, Ik-Mo,Lumbiny, Bilkis Jahan,Taher, Abu
, (2020/07/16)
An amine-functionalized metal organic framework (MOF) was used as highly efficient and recyclable heterogeneous catalyst for Knoevenagel condensation of various aromatic aldehydes and ketones in ethanol. The catalytic efficiency was demonstrated by the hi
A Simple and Highly Versatile Procedure for the Knoevenagel Condensation Promoted by an Efficient, Eco-Friendly, and Recyclable nano-ZnO Catalyst
Alam, M. M.,Asiri, Ya. I.,Sulthana, S. Sh.,Tasqeeruddin, S.
, p. 315 - 321 (2020/04/17)
Abstract: A simple, highly versatile, and efficient protocol for the synthesis of substituted olefins from various aromatic aldehydes and active methylene compounds by Knoevenagel condensation using an efficient, eco-friendly, and recyclable nano-ZnO cata
Ammonium chloride: An efficient and environmentally benign catalyst for knoevenagel condensation of carbonyl and active methylene compounds
Tasqeeruddin,Asiri, Yahya I.,Mujahid Alam
, p. 3024 - 3028 (2021/01/06)
In the present study, a rapid, simple and an efficient procedure for the Knoevenagel condensation of various carbonyl and active methylene compounds in ethanol at a moderate temperature in the presence of a catalytic amount of an efficient, environmentall
