853311-16-7

Upstream product

• 18791-75-8 4-Bromothiophen-2-aldehyde 
• 5720-05-8 4-methylphenylboronic acid 
• 33446-27-4 1-cyclopropyl-1-(p-tolyl)ethanol 
• 624-31-7 4-tolyl iodide 
• 31614-66-1 tributyl(p-tolyl)stannane 
• 106-38-7 para-bromotoluene 

Downstream Products

• 1028303-34-5 (E)-3-[4-(4-methylphenyl)-2-thienyl]acrylic acid chloride 
• 229008-01-9 (E)-3-[4-(4-methylphenyl)-thiophen-2-yl]acrylic acid 

Relevant academic research and scientific papers

Novel method for preparing thiophene formaldehyde compounds

The present invention provides a novel method for preparing thiophene formaldehyde compounds by using cyclopropylethanol and K2S under metal-free catalytic conditions. The thiophene formaldehyde compounds are directly synthesized by using cyclopropylethan

Stannylation of Aryl Halides, Stille Cross-Coupling, and One-Pot, Two-Step Stannylation/Stille Cross-Coupling Reactions under Solvent-Free Conditions

Solvent-free protocols for palladium-catalyzed stannylation of aryl halides, Stille cross-coupling, and one-pot, two-step stannylation/Stille cross-coupling (SSC) are reported for the first time. (Het)aryl halides bearing acceptor, donor, as well as sterically demanding substituents are stannylated and/or coupled in high yields. The reactions are catalyzed by conventional palladium(II) acetate/PCy3 [Pd(OAc)2/PCy3] under air, using available base CsF, and without the use of high purity reagents. The developed synthetic procedures are versatile, robust, and easily scalable. The absence of solvent, and the elimination of isolation procedures of aryl stannanes makes the SSC protocol simple, step economical, and highly efficient for the synthesis of biaryls in a one-pot two-step procedure.

Design and synthesis of natural product derivatives with selective and improved cytotoxicity based on a sesquiterpene scaffold

Brasilamide E (1) is a bisabolane sesquiterpenoid isolated from the solid-substrate fermentation cultures of a plant endophytic fungus Paraconiothyrium brasiliense. The compound specifically inhibited proliferation of the MCF-7 cells, but did not show cyt

Design and synthesis of arylthiophene-2-carbaldehydes via suzuki-miyaura reactions and their biological evaluation

A series of various novel 4-arylthiophene-2-carbaldehyde compounds were synthesized in moderate to excellent yields via Suzuki-Miyaura cross-coupling with different arylboronic pinacol esters/acids. The synthesized products were screened for their antibacterial, haemolytic, antiurease, and nitric oxide (NO) scavenging capabilities and interestingly, almost all products turned out to have good activities. 3-(5-Formylthiophene- 3-yl)-5-(trifloromethyl)benzonitrile (2d) revealed excellent antibacterial activity, showing an IC50 value of 29.7 μg/mL against Pseudomonas aeruginosa, compared to the standard drug streptomycin with an IC50 value 35.2 μg/mL and was also found to be the best NO scavenger, with an IC50 value of 45.6 μg/mL. Moreover, 4-(3-chloro-4-fluorophenyl) thiophene-2-carbaldehyde (2i) exhibited a superior haemolytic action and an outstanding urease inhibition, showing an IC50 value of 27.1 μg/mL.

Non-thiol farnesyltransferase inhibitors: Utilization of the far aryl binding site by arylthienylacryloyl-aminobenzophenones

We recently described two novel aryl binding sites of farnesyltransferase. The 4- and 5-arylsubstituted thienylacryloyl moieties turned out as appropriate substituents for our benzophenone-based AAX-peptidomimetic capable for occupying the far aryl binding site.

Structure-activity relationships of novel anti-malarial agents part 8. Effect of different central aryls in biarylacryloylaminobenzophenones on antimalarial activity

Replacement of the 2,5-disubstituted furyl residue present in the known antimalarial agents 8 by other aryl residues resulted in a more or less reduced antimalarial activity in most cases. The only exemption was the 2,4-thienylene compound 11a displaying activity with an IC50 value of 120 nM. In conclusion, the 2,5-furylene compound 8e remains to represent the most active antimalarial agent in this series of farnesyltransferase inhibitors.