58125-69-2

Upstream product

• 104-47-2 p-methoxybenzylnitrile 
• 64-17-5 ethanol 

Downstream Products

• 141246-09-5 3-[2-(4-Methoxy-benzyl)-5-methyl-benzoimidazol-1-yl]-butyric acid 
• 53039-62-6 2-(4-methoxybenzyl)-1H-benzo[d]imidazole 

Relevant academic research and scientific papers

Colchicine derivatives, and preparation method and medical application thereof

The invention specifically relates to colchicine derivatives (I) as described in the specification and a preparation method thereof, and pharmaceutical compositions containing the colchicine derivatives, belonging to the field of medicinal chemistry. The results of pharmacodynamic experiments prove that the colchicine derivatives of the invention have treatment effect on lumbar disc herniation andliver fibrosis.

Copper(II)-Mediated Aerobic Oxidation of Benzylimidates: Synthesis of Primary α-Ketoamides

A simple and straightforward method for the synthesis of primary α-ketoamides has been discovered. The reaction represents the first example of benzylimidates directly converting to primary α-ketoamides by using sustainable molecular oxygen as an oxidant. This reaction proceeds in the presence of copper(II) salt via cleavage of benzylic C-H and C-O bonds of the benzylimidates with liberation of alcohols as the only byproduct. A wide substrate scope, operationally mild conditions, the use of single substrates, and a reaction scaled up to grams make this strategy very attractive and practical. Furthermore, mechanistic studies illustrate that the imidate group adjacent to the benzylic position plays crucial role in facilitating this chemical process.

Copper(II)-Catalyzed Benzylic C(sp3)-H Aerobic Oxidation of (Hetero)Aryl Acetimidates: Synthesis of Aryl-α-ketoesters

A straightforward method is developed in this paper for the synthesis of α-ketoesters through copper-catalyzed aerobic oxidation of (hetero)aryl acetimidates using molecular oxygen as a sustainable oxidant. The reaction represents the first example of the direct synthesis of aryl-α-ketoesters from arylacetimidates through the aerobic oxidation of a benzylic C(sp3)-H (CO) bond in moderate to good yield. This transformation occurs under mild reaction conditions with a wide range of substrates and utilizes a readily available oxidant and catalyst. The synthetic utility of this transformation is demonstrated through scaled-up synthesis. A plausible reaction mechanism is also proposed.

Antiviral activity of benzimidazole derivatives. III. Novel anti-CVB-5, anti-RSV and anti-Sb-1 agents

A library of eighty-six assorted benzimidazole derivatives was screened for antiviral activity against a panel of ten RNA and DNA viruses. Fifty-two of them displayed different levels of activity against one or more viruses, among which CVB-5, RSV, BVDV a

[(alkoxy)pyridinyl]amine compounds which are useful in the treatment of gastrointestinal disorders

The present invention relates to N-pyridylamidine and N-pyridylguanidine derivatives of general formula (I) in which: Ar1 is an optionally substituted phenyl ring; Ar2 is an optionally substituted phenyl ring; R1 is hydrogen or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 is hydrogen, halogen, C1-6 alkyl or C1-6 alkoxy; X is CH2 or NR5, and R5 is hydrogen or C1-4 alkyl, and the salts thereof, and their use in therapy as gastric acid secretion inhibitors.

Biologically Active Metabolites of Fungi, I.-Isolation, Synthesis, and Biological Activity of Coniothyriomycin as well as Bioassay of Analogous Open-Chain Imides

The mixed open-chain imide N-(3-chloro-4-hydroxyphenylacetyl)fumarate (1), named coniothyriomycin, was isolated as a metabolite of the fungus Coniothyrium.The natural product 1 and the analoguos imides 13-15 and 22-24 have been synthesized by base-catalyzed condensation of the imidates 12a-f with acid chlorides 6a-c or the mixed anhydride 21.The compounds 1 and 13-15 were shown to posess remarkable fungicidal and herbicidal activities in short-termed tests. Key Words: Fungal metabolites / Imides, open-chain / Fungicidal activity / Coniothriomycin

Synthesis and choleretic activity of 3-[2-(3-R', 4-R'', 5-R'''-benzyl)-5- R-benzimidazol-1-yl]-butanoic acids

On the ground of the evidentiated choleretic activity of 3-[2- benzylbenzimidazol-1-yl]butanoic acid, 28 new acids were prepared in order to evaluate the influence of suitable substitutions in either C5 of heteroring or C3', C4', C5' of benzyl group in po

Synthesis and Antiinflammatory Activity of 2,2'-Diaminobiphenyl Derivatives

A series of 2,2'-diaminobiphenyl derivatives was prepared and tested for antiinflammatory activity.Several compounds showed antiinflammatory activity, particularly 2-amino>-2'-amino>biphenyl (4), which als