56106-79-7Relevant academic research and scientific papers
Utility of Complementary Molecular Reactivity and Molecular Recognition (CMR/R) Technology and Polymer-Supported Reagents in the Solution-Phase Synthesis of Heterocyclic Carboxamides
Parlow, John J.,Mischke, Deborah A.,Woodard, Scott S.
, p. 5908 - 5919 (2007/10/03)
The use of our recently reported chemical library purification strategy in the development of a herbicidal lead, N-(3-benzoylphenyl)-3-(1,1-dimethylethyl)-1-methyl-1H-pyrazole-5-carboxamide (3), is described. The approach applying fundamental properties of complementary molecular reactivity and molecular recognition (CMR/R) as the basis for a general purification strategy was utilized. Polymeric reagents were used in the synthesis to generate reactive species involved in product formation, and complementary molecular reactivity/molecular recognition polymer 8 (CMR/R polymer 8) was used in the solution-phase syntheses of building blocks, primary libraries, and lead refinement libraries. An extension of the CMR/R methodology was applied, utilizing a sequestration enabling reagent (SER), transforming a reactant into an electrophilic species sequestrable by CMR/R polymer 8. This library purification strategy enabled rapid lead generation and lead refinement to afford herbicide 27o. The CMR/R solid-phase purification technique enabled a simple, general, and powerful protocol, eliminating the usual tedious and time-consuming methods required for solution-phase product purification. The result was the synthesis of hundreds of compounds, prepared in a relatively short time, leading to a compound with a 4-fold improvement in herbicidal activity over the initial lead.
Diamine-benzophenones and a process for the preparation thereof
-
, (2008/06/13)
New compounds of the general formula (I) SPC1 wherein R1 and R2 each is a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, or R1 and R2 together with the adjacent nitrogen atom may form substituted or unsubstituted heterocyclic group with or without a further oxygen or nitrogen heteroatom, and R3 is hydrogen or an acyl group derived from a C1-18 carboxylic acid. The compounds are prepared by reducing the corresponding nitro compounds of the general formula (II) SPC2 and optionally acylating the obtained product. The compounds of the general formula (I) and their acid addition salts and quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess valuable antipyretic activity and a yohimbine lethality increasing effect characteristic of antidepressants.
