105279-30-9

Upstream product

• 766-98-3 1-ethynyl-4-fluorobenzene 
• 88-67-5 2-Iodobenzoic acid 
• 85-44-9 phthalic anhydride 
• 405-50-5 p-Fluorophenylacetic acid 
• 78610-84-1 1-phenyl-1λ³-benzo[d][1,2]iodaoxol-3(1H)-one 
• 36282-29-8 2'-bromo-2-(p-fluorophenyl)-acetophenone 
• 1864-94-4 phenyl formate 
• 88-65-3 2-bromobenzoic-acid 

Relevant academic research and scientific papers

1-Phenyl-1,2-benziodoxol-3-(1H)-one as Synthon for Phthalide Synthesis through Pd-Free, Base-Free, Sonogashira-Type Coupling Cyclization Reaction

Hypervalent iodine(III) five-membered heterocycles have found broad application as atom-transfer reagents for organic synthesis. Among them, 1-phenyl-1,2-benziodoxol-3-(1H)-one is known as a traditional benzyne precursor, but no further synthetic applicat

Phenylidene phenyl peptide compounds and medicinal composition and application thereof

The invention provides phenylidene phenyl peptide compounds, a medicinal composition using the phenylidene phenyl peptide compounds as active components, and application thereof as monoamine oxidase B(MAO-B) inhibitors and application thereof to preparation of medicines for treating Parkinson's disease (PD). Monoamine oxidase B (MAO-B) has been proved to be closely related to the pathogenesis ofthe Parkinson's disease (PD) and is a classic target for research and development of the medicines for treating the Parkinson's disease (PD). The invention provides application of the phenylidene phenyl peptide compounds to preparation of the monoamine oxidase B (MAO-B) inhibitors. In-vitro kinase activity experiments prove that the phenylidene phenyl peptide compounds have a significant monoamineoxidase B (MAO-B) inhibiting effect.

Palladium-catalyzed carbonylative synthesis of isocoumarins and phthalides by using phenyl formate as a carbon monoxide source

A simple and efficient palladium-catalyzed intramolecular carbonylative synthesis of isocoumarins and phthalides from the easily available starting materials by employing phenyl formate as a CO surrogate has been achieved. The approach affords target compounds in good to excellent yields with the advantages of lower toxicity, milder conditions, easy operation and wide functional group tolerance.

Regioselective one-pot synthesis of isocoumarins and phthalides from 2-iodobenzoic acids and alkynes by temperature control

Copper-catalyzed coupling reaction of 2-iodobenzoic acids and alkynes such as terminal acetylenes, alkynyl carboxylic acids, and trimethylsilylacetylene selectively afforded isocoumarins and phthalides in the presence of cesium carbonate (Cs2CO3) and dimethyl sulfoxide (DMSO). Among the regioselective products, only the 6-endo-dig product, isocoumarin, was formed at 100 °C, and the 5-exo-dig product, phthalide, was formed as a major product at 25 °C. A variety of alkynes produced the corresponding isocoumarins and phthalides in good yields. A mechanism is suggested in which the formation of 2-alkynylbenzoic acid as an intermediate via Sonogashira-type coupling was ruled out in the reaction pathway. Copyright

New method for the synthesis of lactones via nickel-catalyzed isocyanides insertion

A novel nickel catalyst for the reaction of tert-butyl isocyanide insertion was discovered. In this approach, 1,2-bis(diphenylphosphino)ethane (L3) serves as an efficient ligand, thereby allowing the preparation of lactones from (o-bromophenyl)phenylethanone derivatives. It is noteworthy that this is the first example of nickel acting as a metal catalyst in the reactions of tert-butyl isocyanide insertion. The significance of this methodology may draw many chemists attention in the field of isocyanide-incorporating reactions. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]

Pd/C-mediated synthesis of (Z)-3-alkylidenephthalides of potential pharmacological interest

The coupling of o-bromobenzoic acid with terminal alkynes using 10% Pd/C-Et3N-CuI-PPh3 as a catalyst system leads to the synthesis of (Z)-3-alkylidenephthalides as the major product along with the traces of isocoumarin when the reaction was performed in 1,4-dioxane. The methodology afforded a range of compounds including (Z)-3-(4-(methylsulfonyl) benzylidene)isobenzofuran-1(3H)-one of potential pharmacological interest.

Palladium-catalyzed synthesis of isocoumarins and phthalides via tert -butyl isocyanide insertion

A novel and highly efficient strategy for the synthesis of isocoumarins and phthalides through a palladium(0)-catalyzed reaction incorporating tert-butyl isocyanide has been developed. This process, providing one of the simplest methods for the synthesis of this class of valuable lactones, involves two steps including cyclization reaction and simple acid hydrolysis. The methodology is tolerant of a wide range of substrates and applicable to library synthesis.

Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds

The synthesis of several series of imidazo[2,1-a]isoindol-5-ol derivatives and the results of their evaluation against Plasmodium falciparum are presented and discussed. The effects of electron-withdrawing or-donating substituents on different parts of the molecule, as well as those produced by the incorporation of an additional fused ring, were analyzed. Several compounds showed significant antimalarial activity in vitro with IC50 values as low as 60 nM and a certain efficacy in vivo by reducing parasitemia in Plasmodium berghei mouse models.

Synthesis of phthalides via Pd/CNTs-catalyzed reaction of terminal alkynes and o-iodobenzoic acid under copper- and ligand-free conditions

A phosphine- and copper-free protocol for the synthesis of phthalides via Pd/CNTs-catalyzed tandem coupling-cyclization process has been developed. The palladium immobilized on CNTs showed high catalytic activity, and the reactions with a variety of termi