2-Chlorotrityl Chloride and 4-Methylbenzhydryl Bromide Resin Loading Using the Mixture of Organic Solvents: A “Greener” Alternative to Dichloromethane andN,N-Dimethylformamide

• DOI: 10.1021/acs.oprd.1c00356
• Publication Date: 2021-12-27T18:30:48Z
• Authors: Maria Leko; Polina Filippova; Marina Dorosh; Karin Rustler; Thomas Bruckdorfer; Sergey Burov
• Keywords: Dichloromethane; Dimethyl formamide

Common protocols for the loading of 2-CTC and MBH-Br resins presume application DCM, THF, or DMF; these solvents are considered as undesirable in accordance with modern regulatory rules. An alternative option implies usage rather expensive 2-MeTHF. Herein, we describe an EtOAc/AcN (1:1) mixture efficient solvent incorporation first amino acid. We show that suggested reaction conditions ensure a level comparable to 2-MeTHF, DMF. The described procedure was designed kilogram-scale synthesis palmitoyl-hexapeptide.