17910-70-2

Upstream product

• 610-97-9 o-iodo-methyl-benzoic acid 
• 1099102-15-4 methyl 2-((3-methoxyphenyl)ethynyl)benzoate 
• 768-70-7 1-ethynyl-3-methoxybenzene 
• 85-44-9 phthalic anhydride 
• 1798-09-0 m-methoxyphenylacetic acid 
• 88-67-5 2-Iodobenzoic acid 
• 591-31-1 3-methoxy-benzaldehyde 
• 34000-28-7 2'-hydroxy-3-methoxy-chalcone 

Downstream Products

• 1345856-63-4 5-(3-methoxybenzyl)-2,5-dihydro-3H-imidazo[2,1-a]isoindol-5-ol 
• 17910-72-4 2-methoxy-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one 
• 17910-73-5 2-hydroxy-10,11-dihydro-5H-dibenzocyclohepten-5-one 
• 17910-71-3 2-<2-(3-methoxyphenyl)ethyl>benzoic acid 
• 6149-23-1 2-(3-methoxyphenyl)-2H-inden-1,3-dione 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of substituted flavones and aurones as potential anti-influenza agents

We designed a series of substituted flavones and aurones as non-competitive H1N1 neuraminidase (NA) inhibitors and anti-influenza agents. The molecular docking studies showed that the designed flavones and aurones occupied 150-cavity and 430-cavity of H1N1-NA. We then synthesized these compounds and evaluated these for cytotoxicity, reduction in H1N1 virus yield, H1N1-NA inhibition and kinetics of inhibition. The virus yield reduction assay and H1N1-NA inhibition assay demonstrated that the compound 1f (4-methoxyflavone) had the lowest EC50 of 9.36 nM and IC50 of 8.74 μM respectively. Moreover, kinetic studies illustrated that compounds 1f and 2f had non-competitive inhibition mechanism.

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.

Ag2O nanoparticle-catalyzed substrate-controlled regioselectivities: direct access to 3-ylidenephthalides and isocoumarins

Herein, we disclose the first example of an efficient, silver oxide nanoparticle-catalyzed, direct regioselective synthesis of 3-ylidenephthalides 11-16 and isocoumarins 17-20via sonogashira type coupling followed by substrate-controlled 5-exo-dig or 6-endo-dig cyclization reaction, respectively. This one pot coupling involves reaction of substituted 2-halobenzoic acid with meta/para-substituted and ortho-substituted terminal alkynes, which proceeded in a regioselective manner resulting in the formation of 3-ylidenephthalides or isocoumarins, respectively, in excellent yields (up to 95%) with complete Z-selectivity. This protocol features relatively broad substrate scope, mild conditions, operational simplicity, and is favourable with aromatic/alicyclic terminal alkynes. The competition experiments and gram-scale synthesis further highlight the importance and versatility of the methodology. The proposed mechanistic pathways illustrate that the regioselectivity is substantially being controlled by the substituent(s) present on the acetylenic phenyl ring.

Synthesis of isocoumarins: Rhenium complex-catalyzed cyclization of 2-ethynylbenzoic acids

When 2-ethynylbenzoic acids were treated with a catalytic amount of a rhenium complex, such as ReCl(CO)5, 6-endo cyclization of 2-ethynylbenzoic acids proceeded with a high selectivity to give the corresponding isocoumarins in moderate to good yields.

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.

Tricyclic antidepressant derivatives and immunoassay

The present invention is directed to novel tricyclic antidepressant drug derivatives synthesized for covalent attachment to proteins or polypeptide antigens for use in the preparation of antibodies or receptors to tricyclic antidepressant drugs and tricyclic antidepressant metabolites. The new derivatives are characterized by a saturated double bond on the amitriptyline portion of the molecule and are represented by the structure where R1is a saturated or unsaturated, substituted or unsubstituted, straight or branched chain of 0-10 carbon or heteroatoms, X is a linker group consisting of 0-2 substituted or unsubstituted aromatic rings, and Y is an activated ester or NH—Z, where Z is a poly(amino acid). The novel tricyclic antidepressant activated hapten derivatives are useful for preparing tracers and conjugates for tricyclic antidepressant immunoassays, including an enzyme immunoassay and a microparticle capture inhibition assay using an antibody produced from the novel immunogen with a conjugate derivatized either at the N-1 position of imipramine or at the C-2 position of dihydroamitriptyline.

Synthesis of 5--10,11-dihydrodibenzocyclohepten-2-yl>oxy>valeric Acid (CHA) and 5-dibenzocyclohepten-2-yl>oxy>valeric Acid (CHE) Handles for the Solid-Phase Synthesis of C-Terminal ...

Two novel handles for peptide amide preparation under mild conditions were developed for use in highly efficient solid-phase peptide sythesis.These handles, 5--10,11-dihydrodibenzocyclohepten-2-yl>oxy>valeric acid (CHA) and 5-dibenzocyclohepten-2-yl>oxy>valeric acid (CHE), were attached to the solid support and were used for syntheses of peptides having a C-terminal amide by the fluorenylmethoxycarbonyl strategy.The cleavability of CHA and CHE was determined and compared with the that commercially available amide handles.CHA and CHE handles can be rapidly cleaved from the polymer support without significant side reactions using lower acid concentrations than those required for conventional handles.As CHA can be easily synthesized in large amounts, it is suitable for peptide amide preparation for pharmaceuticals.As CHE can be cleaved at very low concentrations of acid, it is especially suitable for preparing side chain-protected peptide amides.Several brain-gut peptides having a C-terminal amide were synthesized in high yield and high purity with these novel handles.

5-Alkyl or hydroxyalkyl substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines and anticonvulsant use thereof

5-Substituted-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imines, derivatives and pharmaceutically acceptable salts thereof are useful as anticonvulsants.

Benzalphthalides and broad spectrum sun screens

Compositions containing a benzalphthalide, i.e. benzalphthalide or a substituted benzalphthalide, are very effective broad spectrum sun screens. They are prepared by reacting substituted or unsubstituted phthalic anhydride with the corresponding substituted or unsubstituted phenyl acetic acid.