Reacción #464193

Ecuación de reacción

DOTA biotin

N-methyl glycine

DOTA biotin

N-methyl-glycine

D-alanine

→

N-methyl glycyl-biotin

Disolventes

DMF

triethylamine

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrowas prepared by an analogous method to

Procedimiento

The N-methyl glycine-linked DOTA-biotin conjugate was prepared by an analogous method to that used to prepare D-alanine-linked DOTA-biotin conjugates. N-methyl-glycine (trivial name sarcosine, available from Sigma Chemical Co.) was condensed with biotin-NHS ester in DMF and triethylamine to obtain N-methyl glycyl-biotin. N-methyl-glycyl biotin was then activated with EDCI and NHS. The resultant NHS ester was not isolated and was condensed in situ with DOTA-aniline and excess pyridine. The reaction solution was heated at 60° C. for 10 minutes and then evaporated. The residue was purified by preparative HPLC to give [(N-methyl-N-biotinyl)-N-glycyl]-aminobenzyl-DOTA.

Fuente