## Abstract An improved method for the preparation of Merrifield resin esters is presented. This method is rapid, is free of racemization, and is not complicated by a quaternization side reaction. Chloromethylated resin beads, __t__‐butoxycarbonyl amino acid, and potassium __t__‐butoxide are heated
A convenient and rapid method for the selective oxygen-17 enrichment of aspartyl peptides during solid-phase synthesis
✍ Scribed by Vassiliki Theodorou-Kassioumis; Nikolaos Biris; Constantinos Sakarellos; Vassilios Tsikaris
- Publisher
- Elsevier Science
- Year
- 2001
- Tongue
- French
- Weight
- 137 KB
- Volume
- 42
- Category
- Article
- ISSN
- 0040-4039
No coin nor oath required. For personal study only.
✦ Synopsis
In this work we describe, for the first time, a rapid and efficient method for 17 O selective labeling on the b-carboxyl group of an aspartic acid residue already incorporated into a peptide sequence anchored on a solid-phase support. The b-O-benzyl ester of the Asp residue of the Ac-RGD-benzydrylamine resin was successfully saponified using Na 17 OH in a methanol/ dichloromethane mixture. The 17 O selective enriched peptide was then released from the solid support by acidic cleavage. The 17 O NMR spectrum confirmed the 17 O labeling of the Asp b-carboxylate.
📜 SIMILAR VOLUMES
1. In the Merrifield solid phase peptide synthesis (l), the benzyl ester attachment of the first amino acid residue to the chloromethylated polystyrene has customarily been effected by heating the polymer, the protected amino acid, and a tertiary amine in an inert solvent at 80" for 48 hours. Bodan
A simple and rapid procedure for the synthesis of AMP"0, AMP'sO, and the corresponding guanosine derivatives is described. The method is based on the intermediate production of P"OC13 or P'\*OClj from PCIs, but does not involve their isolation, so that all steps involved can be carried out in the sa
## Abstract Twelve new 7‐aryl‐3‐cyanopyrazolo[1,5‐__a__]pyrimidines (**3a‐f**) and ethyl 7‐arylpyrazolo[1,5‐__a__]pyrimidine‐3‐carboxylates (**3g‐l**) have been conveniently synthesized by the reaction of enaminones with 5‐amino‐1__H__‐pyrazoles in good yields under microwave irradiation. With one