4530-44-3

Upstream product

• 78957-20-7 3-(hydroxymethyl)phenyl acetate 
• 100-83-4 meta-hydroxybenzaldehyde 
• 108-39-4 3-methyl-phenol 
• 122-46-3 3-acetoxytoluene 
• 34231-78-2 3-formylphenyl acetate 
• 620-24-6 3-Hydroxybenzyl alcohol 
• 108-24-7 acetic anhydride 

Downstream Products

• 1064198-17-9 2-(3-acetoxybenzyl)-7-methoxy-6-triisopropylsilyloxy-1,2,3,4-tetrahydroisoquinoline 

Relevant academic research and scientific papers

Synthesizing method of 4-(4-bromo-3-aldehyde-phenoxyl)-benzonitrile

The invention provides a synthesizing method of 4-(4-bromo-3-aldehyde-phenoxyl)-benzonitrile. The synthesizing method comprises the following steps of using 3-methylphenol as the starting raw material, and reacting with acid anhydride to prepare 3-methyl-benzene ester; enabling the 3-methyl-benzene ester and sulfonyl chloride to react, so as to prepare a mixture of 3-chloromethyl-benzene ester and3-dichloromethyl-benzene ester; adding ulotropine, and hydrolyzing, so as to obtain 3-hydroxyl-benzaldehyde; performing brominating reaction, so as to obtain 4-bromo-3-hydroxyl-benzaldehyde; adding 4-fluorobenzonitrile, and performing condensation reaction, so as to obtain the 4-(4-bromo-3-aldehyde-phenoxyl)-benzonitrile. The synthesizing method has the advantages that the prices of the reactionraw materials are low, the obtaining is easy, the reaction steps are fewer, the production cost is low, the technology is simple, the product purity is high and reaches 99.0% or above, and the synthesizing method is suitable for industrialized production.

Chemical insights in the concept of hybrid drugs: The antitumor effect of nitric oxide-donating aspirin involves a quinone methide but not nitric oxide nor aspirin

Hybrid drug 1 (NO-ASA) continues to attract intense research from chemists and biologists alike. It consists of ASA and a -ONO2 group connected through a spacer and is in preclinical development as an antitumor drug. We report that, contrary to current beliefs, neither ASA nor NO contributes to this antitumor effect. Rather, an unsubstituted QM was identified as the sole cytotoxic agent. QM forms from 1 after carboxylic ester hydrolysis and, in accordance with the HSAB theory, selectively reacts with cellular GSH, which in turn triggers cell death. Remarkably, a derivative lacking ASA and the -ONO 2 group is 10 times more effective than 1. Thus, our data provide a conclusive molecular mechanism for the antitumor activity of 1. Equally importantly, we show for the first time that a "presumed invisible" linker in a hybrid drug is not so invisible after all and is in fact solely responsible for the biological effect.

Thiadiazole derivatives for the treatment of depressive states

Thiadiazole derivatives of general formula (I) wherein R1 is selected from the class consisting of: C1-C10 linear or branched alkyl, benzyl, optionally substituted at the aromatic ring with one or more groups se