4785-56-2

Upstream product

• 5486-55-5 2,6-dimethoxylnaphthalene 
• 3469-26-9 2,7-Dimethoxynaphthalene 
• 41634-29-1 4-methoxybenzocyclobutene-1,2-dione 
• 7732-18-5 water 
• 40125-47-1 3-Bromo-6-methoxy-3H-isobenzofuran-1-one 
• 1711-05-3 m-anisoyl chloride 
• 1570134-65-4 N-(2-(4,5-dihydrooxazol-2-yl)phenyl)-3-methoxybenzamide 
• 68-12-2 N,N-dimethyl-formamide 
• 22921-68-2 2-bromo-5-methoxy-benzoic acid 
• 586-38-9 3-Methoxybenzoic acid 
• 4741-63-3 6-methoxyphthalide 

Downstream Products

• 60889-22-7 7-methoxyphthalazin-1-(2H)-one 
• 871502-92-0 2-bis(5-methyl-2-furyl)methyl-5-methoxybenzoic acid 
• 871502-99-7 {2-[bis-(5-methyl-furan-2-yl)-methyl]-5-methoxy-phenyl}-methanol 
• 85370-63-4 N,N-diethyl-2-formyl-5-methoxybenzamide 
• 1374150-54-5 ethyl 2-formyl-5-methoxybenzoate 
• 1374149-87-7 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-5-methoxy-N-methyl-benzamide 
• 1374150-55-6 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-5-methoxy-N-methyl-benzamide 
• 1221486-42-5 2-(3-acetamidophenethyl)-5-methoxybenzoic acid 
• 77620-05-4 methyl 5-methoxyl-2-formylbenzoate 
• 1605303-06-7 2-benzyl-3-(1H-indol-3-yl)-6-methoxyisoindolin-1-one 
• 1011029-55-2 (E)-2-[2-(3-chlorophenyl)vinyl]-5-methoxybenzoic acid 

Relevant academic research and scientific papers

Cell-Trappable BODIPY-NBD Dyad for Imaging of Basal and Stress-Induced H2S in Live Biosystems

H2S is a gaseous signaling molecule that is involved in many physiological and pathological processes. In general, the level of intracellular H2S (1 μM) is much lower than that of GSH (～1–10 mM), leading to the remaining challenge o

Indium-Catalyzed C?F Bond Transformation through Oxymetalation/β-Fluorine Elimination to Access Fluorinated Isocoumarins

Fluorinated heterocycles have attracted much attention in the pharmaceutical and agrochemical industries. Many strategies have already been developed to achieve the synthesis of fluorinated heterocycles. Formidable challenges remain, however, in the synthesis of fluorinated isocoumarin derivatives that are among the most alluring structural motifs. Herein, the indium-catalyzed C?F bond transformation of 2-(2,2-difluorovinyl) benzoates is reported, which are readily accessible compounds, to give a diverse array of fluorinated isocoumarins. The present reaction proceeds smoothly using inexpensive reagents: a catalytic amount of indium salt in the presence of zinc salt. A theoretical calculation of potential energy profiles showed that the reaction consists of oxymetalation with the elimination of alkyl halide and the β-fluorine elimination.

Cu-Catalyzed C-H Alkenylation of Benzoic Acid and Acrylic Acid Derivatives with Vinyl Boronates

An efficient Cu-catalyzed C-H alkenylation with acyclic and cyclic vinyl boronates was realized for the first time under mild conditions. The scope of the vinyl borons and the compatibility with functional groups including heterocycles are superior than Pd-catalyzed C-H coupling with vinyl borons, providing a reliable access to multisubstituted alkenes and dienes. Subsequent hydrogenation of the product from the internal vinyl borons will lead to installation of secondary alkyls.

SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS, ANALOGUES THEREOF, AND METHODS USING SAME

The present invention includes substituted 3,3'-bis(phenoxymethyl)-1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient.

Sterically Shielded, Stabilized Nitrile Imine for Rapid Bioorthogonal Protein Labeling in Live Cells

In pursuit of fast bioorthogonal reactions, reactive moieties have been increasingly employed for selective labeling of biomolecules in living systems, posing a challenge in attaining reactivity without sacrificing selectivity. To address this challenge, here we report a bioinspired strategy in which molecular shape controls the selectivity of a transient, highly reactive nitrile imine dipole. By tuning the shape of structural pendants attached to the ortho position of the N-aryl ring of diaryltetrazoles-precursors of nitrile imines, we discovered a sterically shielded nitrile imine that favors the 1,3-dipolar cycloaddition over the competing nucleophilic addition. The photogenerated nitrile imine exhibits an extraordinarily long half-life of 102 s in aqueous medium, owing to its unique molecular shape that hinders the approach of a nucleophile as shown by DFT calculations. The utility of this sterically shielded nitrile imine in rapid (～1 min) bioorthogonal labeling of glucagon receptor in live mammalian cells was demonstrated.

Chiral 3-substituted isoindolinone compounds, and preparation method and application thereof

The invention discloses chiral 3-substituted isoindolinone compounds, and a preparation method and application thereof. The compounds are as shown in a formula I which is described in the specification. The preparation method comprises a step of subjecting a compound as shown in a formula II and a compound as shown in a formula III to a Ugi two-component four-center reaction or subjecting a compound as shown in a formula IV, a compound as shown in a formula V and the compound as shown in the formula III to a Ugi three-component four-center reaction in the presence of a chiral phosphoric acid catalyst so as to obtain the compounds as shown in the formula I after completion of the reactions. According to the invention, extensively available raw materials and the cheap and easily available chiral catalyst are used; the raw materials are subjected to the Ugi two-component four-center reaction or the Ugi three-component four-center reaction so as to efficiently prepare the chiral 3-substituted isoindolinone compounds in one step; reaction conditions are mild; and the prepared compounds are stable in the air, high in yield, good in enantioselectivity and easy to separate and purify, and have good application prospects.

TiCl4-Mediated Preparation of Thiophthalide Derivatives via Formal Thio-Passerini Reactions

By the formal extension of the Passerini reaction to thiocarbonyl derivatives, the straightforward preparation of thiophthalides is disclosed. This method involves the intermediate formation of a sulfanyl-phthalide and a titanium tetrachloride mediated is

Highly enantioselective synthesis of 2,3-dihydro-1 H-imidazo[2,1-a isoindol-5(9b H)-ones via catalytic asymmetric intramolecular cascade imidization-nucleophilic addition-lactamization

Highly enantioselective catalytic asymmetric intramolecular cascade imidization-nucleophilic addition-lactamization of N1-alkylethane-1,2-diamine with methyl 2-formylbenzoate catalyzed by a chiral phosphoric acid represents the first efficient method for the preparation of medicinally interesting chiral 2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-ones with high yields and excellent enantioselectivities. This strategy has been shown to be quite general toward various methyl 2-formylbenzoates.

A synthetic route to chiral C(3)-functionalized phthalides via a Ag(I)-catalyzed allylation/transesterification sequence

A Ag(I)-catalyzed synthesis of chiral C(3)-substituted phthalides (8a-f) via a Sakurai-Hosomi allylation/transesterification reaction is described (ee ≤86%). A notable feature of this reaction is that it utilizes ortho-substituted aldehydes, which are a class of compounds that generally afford poor levels of stereoinduction when applying most known catalytic asymmetric allylation approaches. It was also found that elongation of the n-alkyl chain length (R1, up to n=6; R2=H) of the starting alkyl 2-formylbenzoates (7g-i) improved the enantiomeric excess (ee) of the product.

DIBENZOCYCLOHEPTATONE DERIVATIVES AND PHARMACEUTICAL AGENTS CONTAINING SAID COMPOUNDS

The present invention relates to compounds of the formula I wherein R1, R2, R3, R4, X and Y have the meanings given in the description. The compounds have an action which is immunomodulating and inhibits or regulates the release of IL-1β and/or TNF-α. The