Acrylamide derivatives as antiallergic agents. III. Synthesis and structure-activity relationships of N-(4-(4-diphenylmethyl-1-piperazinyl)butyl)- and N-(4-(4-diphenylmethylene-1-piperidyl)butyl)-3-heteroacrylacrylamides.

Synthesis of Some <i>N</i>-[(4-Substituted-1-Piperazinyl)-Oxo(Alkyl and Ethylcarbamoyl)]-3-(2-Thiophenyl)Acrylamides as Non-Steroidal Anti-Allergic and Anti-Inflammatory Agents

“…Traditionally symptomatic treatment of allergies and bronchial asthma has been provided by β-sympathomimetic agents, methylxanthines, corticosteroids, and anticholinergics [1][2][3]. Japanese authors have synthesized a series of acrylamide derivatives linked with different piperazines via alkyl chains and proved them as promising anti-allergic candidates (Figure 1(A)) [4][5][6][7].…”

A Preparative Route to Methyl 3-(Heteroaryl)acrylates Using Heck Methodology

“…We needed to prepare a number of methyl 3-(heteroaryl)acrylates for use as intermediates for the production of pharmaceutical scaffolds. Surprisingly the reaction failed when run under the standard Heck conditions . For example, the reaction of 5-bromopyrimidine with methyl acrylate using triphenylphosphine yielded none of the desired product 4e.…”

“…Surprisingly the reaction failed when run under the standard Heck conditions . For example, the reaction of 5-bromopyrimidine with methyl acrylate using triphenylphosphine yielded none of the desired product 4e. An alternate approach using acrylic acid in the place of methyl acrylate under standard Heck conditions at 160 °C followed by esterification of the crude product with methanol/HCl afforded the product in a disappointing 25% overall yield (Scheme ).…”