Investigation of the labelling characteristics of 99mTc-mercaptoacetyltriglycine

Benzamidomethylation with (Benzamidomethyl)triethylammonium Chloride. 2. A Simple Method for Benzamidomethylation of Thiols, Amines and Carboxylic Acids

“…Also, 5g formed when a large quantity of TEA was added to the aqueous reaction mixture of 1 or an aqueous mixture of 1 and any other nucleophilic substrate (phenols, thiols, etc). A possible explanation for this phenomena is that pure TEA (98%) contains some quantity of NH 3 . The physicochemical data of compounds 5a-h are given in Table 2, and their 1 H-NMR and 13 C-NMR data are given in Table 3.…”

“…A solution of 1 (2.8611 g, 10.59 mmol) in water (40 cm 3 ) was added to the water (40 cm 3 ) mixture of 2a (0.538 g, 5.7 mmol) and TEA (0.3-0.5 cm 3 ). The mixture was stirred for 1h at room temperature.…”

“…Mixture of 1 (2.5633 g, 9.46 mmol), 2g (0.9758 g, 7.99 mmol) and TEA (0.2-0.4 cm 3 ) in CHCl 3 (40 cm 3 ) was refluxed for 20-30 min. The solvent was removed under reduced pressure and theresidue was dissolved in dioxane.…”

“…In the final decade, in the case of a thiol group, benzamidomethylation was used for synthesis of ligands for 99 Tc complexes, which have been utilized as radiolabels [2][3][4]. Also, benzamidomethylation was used to obtain some benzamidomethyl aryl thioethers as intermediates in the synthesis of benzothiazines [5][6][7].…”

In Vivo Evaluation of Cysteine-Based Chelators for Attachment of 99mTc to Tumor-Targeting Affibody Molecules

“…George and co-workers (24) have reported that labeling of scFv containing the GGGC sequence provided higher labeling yields (about 97%) in an alkaline condition. Alkaline pH is usually favorable for rapid 99m Tc-labeling, probably because of deprotonation of sulfur and nitrogen donor atoms, which facilitates the complexation of technetium (35,36). The direct labeling method in alkaline solution (0.15 M NaOH, pH ∼ 11) provided a high radiochemical yield (90%), and a stable technetium labeling was achieved.…”