RESUMEN
Simultaneous structuro-kinetic information obtained via time resolved stopped-flow/UV-Vis spectroscopy/dispersive EXAFS (EDE) experiments elucidated a two-step process for the addition of iodobenzene to [(Ph3P)2Pd(dba)].
RESUMEN
The identification of an agent that is selectively activated by a cytochrome P450 (CYP) has the potential for tissue specific dose intensification as a means of significantly improving its therapeutic value. Towards this goal, we disclose evidence for the pathway of activation of a duocarmycin analogue, ICT2700, which targets CYP1A1 for biological activity.
Asunto(s)
Alquilantes/farmacología , Citocromo P-450 CYP1A1/metabolismo , Citotoxinas/farmacología , Indoles/farmacología , Alquilantes/química , Animales , Biotransformación , Células CHO , Cricetinae , Cricetulus , Citocromo P-450 CYP1A1/genética , Citotoxinas/química , Humanos , Indoles/química , Terapia Molecular Dirigida , Oxidación-ReducciónRESUMEN
This tutorial review deals with recent advances in the use of phosphine-functionalised polymers in organic synthesis. In the first part of the review, some recent applications of polymer-supported palladium catalysts are reviewed, particularly recyclable catalysts for C-C and C-X bond formation with aryl bromide and chloride substrates. In the second half, novel applications of phosphine-functionalised polymers as reagents, scavengers, organocatalysts and linkers in organic chemistry are presented. Emphasis is placed on the synthesis of biologically active molecules.
Asunto(s)
Compuestos Orgánicos/síntesis química , Compuestos Organometálicos/química , Fosfinas/química , Polímeros/química , Catálisis , Estructura Molecular , Compuestos Orgánicos/química , EstereoisomerismoRESUMEN
Optically active torcetrapib was synthesized in seven steps from achiral precursors without the need for protecting groups, utilizing an enantioselective aza-Michael reaction to achieve asymmetry.
Asunto(s)
Química Orgánica/métodos , Quinolinas/química , Quinolinas/síntesis química , Aminoácidos/química , Carbamatos/química , Catálisis , Modelos Químicos , Conformación Molecular , Estructura Molecular , Estereoisomerismo , Factores de TiempoRESUMEN
Merrifield resin was functionalised with hydroxybenzaldehyde under microwave irradiation. The resultant resin was used as a means for immobilisation and activation of alpha-amino acid esters for alkylation reactions. Alpha,alpha-disubstituted and cyclic amino acid esters were prepared in good yields.
Asunto(s)
Aldehídos/química , Aminoácidos/síntesis química , Ésteres/síntesis química , Resinas Sintéticas/química , Aldehídos/efectos de la radiación , Microondas , Estructura Molecular , Resinas Sintéticas/efectos de la radiaciónRESUMEN
The regeneration and reuse of a supported scavenger 1 for amine sequestration has been achieved up to three times without significant loss of activity. The scavenging process between the aldehyde resin 1 and a range of amines has been investigated in detail to determine the scope of this scavenger. Its application for the rapid purification of a small library of secondary amines 7a-j has also been demonstrated, and it has been shown that the large excess of scavenger resin used can be recovered and recycled, making this a more cost-effective process.