91843-55-9

Upstream product

• 623-73-4 diazoacetic acid ethyl ester 
• 2039-82-9 1-bromo-4-ethenyl-benzene 
• 82665-91-6 α,α-diiodoethylacetate 
• 100115-96-6 4-Chlor-4-(4-brom-phenyl)-buttersaeureethylester 
• 24393-53-1 ethyl (E)-3-(4-bromophenyl)-2-propenoate 
• 36501-44-7 (Diethylamino)dimethyloxosulfonium tetrafluoroborate 
• 186581-53-3 diazomethane 
• 1122-91-4 4-bromo-benzaldehyde 
• 1774-47-6 trimethylsulfoxonium iodide 
• 65591-79-9 (E)-1-(4-Bromo-phenyl)-pent-1-en-3-one 
• 1200-07-3 trans-4-bromocinnamic acid 
• 24393-53-1 ethyl 4-bromocinnamate 
• 420-04-2 CYANAMID 
• 1885-28-5 γ-(4-bromophenyl)-γ-butyrolactone 

Downstream Products

• 114095-64-6 (1S*, 2S*)-(2-(4-bromophenyl)cyclopropyl)methanol 
• 1418287-95-2 (±)-trans-O-tert-butyl-N-(2-(4-bromophenyl)cyclopropyl)carbamate 
• 1119807-15-6 C₁₁H₉NO₂ 
• 132145-60-9 ethyl trans-2-(p-cyanophenyl)-1-cyclopropanecarboxylate 

Relevant academic research and scientific papers

NOVEL LYSOPHOSPHATIDIC ACID DERIVATIVE

PROBLEM TO BE SOLVED: To provide a compound that specifically activates an LPA4 receptor, and a pharmaceutical composition containing the same. SOLUTION: This invention relates to a novel lysophosphatidic acid derivative that has an agonistic action on an LPA4 receptor and is useful for the prevention and/or treatment of a disease with angiodysplasia caused by the LPA4 receptor, or a disease associated with angiopathy, or symptoms associated therewith. This invention also relates to a pharmaceutical composition containing the lysophosphatidic acid derivative. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

Aryl alkylamine compound, preparation method thereof and application of aryl alkylamine compound in medicines

The invention relates to an aryl alkylamine compound, a preparation method thereof and application of the aryl alkylamine compound in medicines. Particularly, the compound disclosed by the invention is suitable for being used as a calcium-sensitive recept

Iron/N-doped graphene nano-structured catalysts for general cyclopropanation of olefins

The first examples of heterogeneous Fe-catalysed cyclopropanation reactions are presented. Pyrolysis of in situ-generated iron/phenanthroline complexes in the presence of a carbonaceous material leads to specific supported nanosized iron particles, which are effective catalysts for carbene transfer reactions. Using olefins as substrates, cyclopropanes are obtained in high yields and moderate diastereoselectivities. The developed protocol is scalable and the activity of the recycled catalyst after deactivation can be effectively restored using an oxidative reactivation protocol under mild conditions. This journal is

Regioselective Br?nsted Acid-Catalyzed Annulation of Cyclopropane Aldehydes with N′-Aryl Anthranil Hydrazides: Domino Construction of Tetrahydropyrrolo[1,2- a]quinazolin-5(1 H)ones

A highly regioselective synthesis of tetrahydropyrrolo[1,2-a]quinazolin-5(1H)one derivatives was achieved by reacting cyclopropane aldehydes with N′-aryl anthranil hydrazides in the presence of p-toluene sulfonic acid (PTSA). The transformation involves domino imine formation and intramolecular cyclization to form 2-arylcyclopropyl-2,3-dihydroquinolin-4(1H)-one, followed by nucleophilic ring opening of the cyclopropyl ring to form desired tetrahydropyrrolo[1,2-a]quinazolin-5(1H)one in good to excellent yield with complete regioselectivity. This protocol tolerates a great variety of functional groups and thus provides a simple and step-efficient method for pyrroloquinazolinone synthesis.

A transition-metal-free & diazo-free styrene cyclopropanation

An operationally simple and broadly applicable novel cyclopropanation of styrenes using gem-diiodomethyl carbonyl reagents has been developed. Visible-light triggered the photoinduced generation of iodomethyl carbonyl radicals, able to cyclopropanate a wide array of styrenes with excellent chemoselectivity and functional group tolerance. To highlight the utility of our photocyclopropanation, we demonstrated the late-stage functionalization of biomolecule derivatives.

Au Nanoparticle-Catalyzed Silaboration of Aryl-Substituted Cyclopropyl Aldehydes Forming Rearranged β-Boronate Silyl Enol Ethers

2-Aryl-substituted cyclopropyl aldehydes undergo an unprecedented Au nanoparticle-catalyzed silaboration leading to rearranged linear β-boronate-bearing silyl enol ethers. Formation of these products is attributed to the ring opening radical clock rearran

Generation and Reactivity of Electron-Rich Carbenes on the Surface of Catalytic Gold Nanoparticles

The reactive nature of carbenes can be modulated, and ultimately reversed, by receiving additional electron density from a metal. Here, it is shown that Au nanoparticles (NPs) generate an electron-rich carbene on surface after transferring electron density to the carbonyl group of an in situ activated diazoacetate, as assessed by Fourier transformed infrared (FT-IR) spectroscopy, magic angle spinning nuclear magnetic resonance (MAS NMR), and Raman spectroscopy. Density functional theory (DFT) calculations support the observed experimental values and unveil the participation of at least three different Au atoms during carbene stabilization. The surface stabilized carbene shows an extraordinary stability against nucleophiles and reacts with electrophiles to give new products. These findings showcase the ability of catalytic Au NPs to inject electron density in energetically high but symmetrically allowed valence orbitals of sluggish molecules.

Exploitation of Cyclopropane Carbaldehydes to Prins Cyclization: Quick Access to (E)-Hexahydrooxonine and Octahydrocyclopenta[ b]pyran

A single-step TiX4-mediated Prins-type cyclization of cyclopropane carbaldehydes with 3-buten-1-ol for the highly stereoselective construction of relatively strained (E)-hexahydrooxonines is reported. Switching the alcohol to 3-butyn-1-ol prompted a similar route, augmented by another cyclization within a nine-membered ring to afford a bicyclized product (4,4-dihalo-5-aryloctahydrocyclopenta[b]pyran). Easy transformation of the resulting geminal dihalide to a vinyl halide and a ketone further supplemented the substance of this approach.

Synthesis and in vitro evaluation of novel N-cycloalkylcarbamates as potential cholinesterase inhibitors

Abstract: This present paper describes the preparation and characterization of a series of O-substituted N-cycloalkylcarbamate derivatives. These compounds were tested as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). All studied carbamates exhibited moderate inhibitory activity of both cholinesterases with values of IC50 in the range of 36.1–78.6?μM for AChE and 9.8–215.4?μM for BChE, respectively. These values are comparable with those values of inhibition obtained with the established drug rivastigmine. The cytotoxicity of all carbamates was evaluated using standard in vitro test with Jurkat cells. Many of the studied carbamates can be considered as promising compounds for potential medicinal applications with regard to their inhibitory activity as well as negligible cytotoxicity.

Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy

GPR120 agonists have therapeutic potential for the treatment of diabetes, but few selective agonists have been reported. We identified an indazole-6-phenylcyclopropylcarboxylic acid series of GPR120 agonists and conducted SAR studies to optimize GPR120 potency. Furthermore, we identified a (S,S)-cyclopropylcarboxylic acid structural motif which gave selectivity against GPR40. Good oral exposure was obtained with some compounds displaying unexpected high CNS penetration. Increased MDCK efflux was utilized to identify compounds such as 33 with lower CNS penetration, and activity in oral glucose tolerance studies was demonstrated. Differential activity was observed in GPR120 null and wild-type mice indicating that this effect operates through a mechanism involving GPR120 agonism.