37183-61-2

Upstream product

• 3054-95-3 acrylaldehyde diethyl acetal 
• 20469-63-0 1-iodo-2,4-dimethoxybenzene 
• 75-07-0 acetaldehyde 
• 613-45-6 2,4-Dimethoxybenzaldehyde 
• 1363130-07-7 o,p-dimethoxycinnamyl alcohol 
• 17715-69-4 1-Bromo-2,4-dimethoxybenzene 
• 151-10-0 1,3-Dimethoxybenzene 
• 127921-20-4 1-((E)-3,3-Diethoxy-propenyl)-2,4-dimethoxy-benzene 
• 89691-57-6 1-(2,4-dimethoxyphenyl)ethan-1-ol 
• 68-12-2 N,N-dimethyl-formamide 
• 624-67-9 Propargylic aldehyde 

Downstream Products

• 1380293-90-2 (E)-1-(2,4-dimethoxyphenyl)hexa-1,5-dien-3-ol 
• 1380294-06-3 (E)-6-(2,4-dimethoxystyryl)-5,6-dihydro-2H-pyran-2-one 
• 1380293-98-0 (E)-1-(2,4-dimethoxyphenyl)hexa-1,5-dien-3-yl acrylate 
• 1380294-23-4 (E)-6-(2,4-dimethoxystyryl)-5,6-dihydropyridin-2(1H)-one 
• 1380294-15-4 (E)-N-(1-(2,4-dimethoxyphenyl)hexa-1,5-dien-3-yl)-acrylamide 

Relevant academic research and scientific papers

Discovery of novel diphenylbutene derivative ferroptosis inhibitors as neuroprotective agents

Ferroptosis is a regulated and iron-dependent cell death. Ferroptosis inhibitors are promising for treating many neurological diseases. Herein, with phenotypic assays, we discovered a new diphenylbutene derivative ferroptosis inhibitor, DPT. Based on this hit, we synthesized fourteen new diphenylbutene derivatives, evaluated their ferroptosis inhibitory activities in HT22 mouse hippocampal neuronal cells, and found that three compounds exhibited improved inhibitory activities compared with DPT. Among these active compounds, compound 3f displayed the most potent anti-ferroptosis activity (EC50 = 1.7 μM). Further studies demonstrated that 3f is a specific ferroptosis inhibitor. And we revealed that different from the classic ferroptosis inhibitors, 3f blocked ferroptosis by increasing FSP1 protein level. Moreover, 3f can penetrate blood-brain barrier (BBB). In a rat model of ischemic stroke, 3f effectively mitigated cerebral ischemic injury. Therefore, we are confirmed that 3f, as a novel ferroptosis inhibitor with a new scaffold, is promising for further development as an agent against neurological diseases.

One-Pot Preparation of (E)-α,β-Unsaturated Aldehydes by a Julia-Kocienski Reaction of 2,2-Dimethoxyethyl PT Sulfone Followed by Acid Hydrolysis

(E)-α,β-Unsaturated aldehydes were synthesized by the Julia-Kocienski reaction of 2,2-dimethoxyethyl 1-phenyl-1H-tetrazol-5-yl (PT) sulfone 3 with various aldehydes, followed by acid hydrolysis. The reaction could be carried out in one pot, and various (E)-α,β-unsaturated aldehydes were obtained in a short time and with high yields.

Dihydropyrimidinones: Efficient one-pot green synthesis using Montmorillonite-KSF and evaluation of their cytotoxic activity

A simple, efficient, cost-effective, recyclable and green approach has been developed for the synthesis of new dihydropyrimidinone analogs via the Biginelli reaction. The methodology involves a multicomponent reaction catalyzed by "HPA-Montmorillonite-KSF"as a reusable and heterogeneous catalyst. This method gives an efficient and much improved modification of the original Biginelli reaction, in terms of yield and short reaction times under solvent free conditions. All the derivatives were subjected to cytotoxicity screening against a panel of four different human cancer cell lines viz. colon (Colo-205), prostate (PC-3), leukemia (THP-1) and lung (A549) to check their effect on percentage growth. MTT [3-(4,5-dimethylthiazol-yl)-diphenyl tetrazoliumbromide] cytotoxicity assay was employed to check IC50 values. Of the synthesized analogs, 16a showed the best activity with IC50 of 7.1 ± 0.8, 13.1 ± 1.4, 13.8 ± 0.9 and 14.7 ± 1.1 μM against lung (A549), leukemia (THP-1), prostate (PC-3) and colon (Colo-205) cancer lines, respectively. The 16a analog was further checked for its effect on cancer cell properties through clonogenic (colony formation) and scratch motility (wound healing) assays and thereby was found that it reduced both the colony formation and migratory properties of the lung cancer cell line (A549). Further, molecular docking studies were performed with 16a to show its binding mode. This journal is

Diarylheptanoid compound

The invention discloses a diarylheptanoid compound shown as a formula (A). The compound provided by the invention can be used for remarkably inhibiting transcription and protein expression of iNOS, IL-1beta and IL-6 and a phosphorylation level of IkappaB protein, and can be used for treating inflammation and other various diseases including ichorrhemia and Alzheimer disease. (The formula (A) is shown in the description.).

Stabilization and activation of unstable propynal in the zeolite nanospace and its application to addition reactions

Propynal (HC≡C-CHO), having both a C≡C triple bond and a formyl group in a molecule, is a promising building block but its labile property to easily polymerize often narrows its application for organic synthesis. In a similar way to unstable molecules, such as formaldehyde and acrolein, propynal is also stabilized and remains unchanged in supercages of Na-Y zeolite for over 30 days at ambient temperature. There, the carbonyl oxygen atoms of propynal coordinate to sodium ions in Na-Y which was proved by a 13C-DD/MAS-NMR analysis. In addition, propynal adsorbed in zeolite is sufficiently activated to allow unprecedented reactions; i.e., (1) a 1,3-dipolar cycloaddition with electron-deficient α-diazocarbonyl compounds, (2) a 1,4-addition with mono-, di-, and trimethoxy-substituted benzenes, and (3) a [2 + 2] cycloaddition of unactivated cycloalkenes. The nanospace of the zeolites keeps the products from dimerization during reaction (1) and from successive side-reactions in reaction (2). Quantum chemical calculations demonstrated that reaction (3) proceeds via a one-step-like non-concerted mechanism to afford the corresponding [2 + 2] cycloadducts. These three reactions can produce valuable synthetic intermediates retaining both a formyl group and a C=C double bond.

Synthesis of methoxylated goniothalamin, aza-goniothalamin and γ-pyrones and their in vitro evaluation against human cancer cells

The present work describes the preparation of three novel series of compounds based on the structure of goniothalamin, a natural styryl lactone which has been found to display cytotoxic and antiproliferative activities against a variety of cancer cell lines. A focused library of 29 novel goniothalamin analogues was prepared and evaluated against seven human cancer cell lines. While the γ-pyrones and the aza-goniothalamin analogues were less potent than the lead compound, 2,4-dimethoxy analogue 88 has shown to be more potent in vitro than goniothalamin against all cancer cell lines evaluated. Furthermore, it was more potent than doxorubicin against NCI-ADR/RES, OVCAR-03 and HT-29 while being less toxic to human keratinocytes (HaCat). The 3,5-dimethoxy analogue 90 and 2,4,5-trimethoxy analogue 92 also displayed promising antiproliferative activity when compared to goniothalamin (1). These results provide new elements for the design and synthesis of novel representatives of this family of natural compounds.

1-Tributylstannyl-3,3-diethoxyprop-1-ene as a d3 Acrolein Equivalent

1-Tributylstannyl-3,3-diethoxyprop-1-ene has proved to be a readily available β-formylvinyl anion equivalent which under mild experimental conditions gives ready access to cinnamic skeletons and 4-oxo- or 6-oxo-α,β-enals.