CHEMICAL SYNTHESIS

Chemical Synthesis

Introduction

Taking advantage of our chemistry-based methodology to construct a novel SPOS (solid phase organic synthesis) resins, triazolylmethyl related catechol 6a was found that easily available via copper (I)-catalyzed azide-alkyne cycloaddition (CuAAC) from azidomethyl substituted polystyrene O-propargylcatechol and can be used for parallel synthesis of N-phenyltriazole carboxamides(Dough 2010). As a proof of concept, strategy "catch and release" can be successfully applied for parallel synthesis of dopaminergic phenyltriazoles type 2.

Purpose

Since the relevant layout display the optimum reactivity and the tumor is crucial for success, we have prepared a new functionalized resin, using the concept of chemistry. Thus, CuAAC of alkynyl-substituted pen with azidomethyl polystyrene led to a new family of high BAL (backbone amide linker), 4 REM (regenerative Michael acceptor), SPAN (solid / solution-phase annulation) and scavenger resins. "Pitches" including solid phase supported reactions to work under almost ideal conditions meet the requirements of chemistry(Hepworth 2007).

Goal

Dopamine D3 receptor attracts great attention as a potential target for drugs as selective D3 ligands are promising agents for the treatment of schizophrenia, Parkinson's disease and drug abuse. Extensive research and structure-activity showed that the aryl carboxamides bearing N-alkyl-N'-arylpiperazine side chain exhibit preferential D3 recognition.,,, And, using our chemistry-based resins BAL, we reported on the parallel synthesis of biphenyl carboxamides Type 1A and N-benzyl-1 ,2,3-triazole carboxamides of type 1b. To further optimize the receptor profiles, we wanted to approach the structural hybrids of type 2 changes are described N-benzyltriazole based ligands to the N-phenyl substituted derivatives.

 

Changes

Unfortunately, developed a framework amide linker strategy, including [3 +2] cycloaddition strong support propynoic amide acid benzyl azide cannot be used for construction phenyltriazoles so busy arylazides expanded at the required temperature from 0 ° C.

In contrast to previously used phenylthioethers link catch and release features, we try to take advantage of supposedly chemically more stable phenylether based oxa-analogs ...