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Methods of Protein Iodination
Published in Erwin Regoeczi, Iodine-Labeled Plasma Proteins, 2019
The method takes its origin from an observation made in peptide synthesis, namely, that because of the water solubility of N-hydroxysuccinimide, the resulting esters are more convenient to use than those of N-hydroxyphthalimide.136 The ester bond between the propionic acid and the hydroxyimide can be established136,137 by the carbodiimide technique, e. g., by using dicyclohexylcarbodiimide, with approximately one third yield. The ester is also available commercially. Its molecular weight (before halogenation) is 263.25.
Evaluation of WO2014121383 A1: a process for preparation of rufinamide and intermediates
Published in Expert Opinion on Therapeutic Patents, 2019
Barnali Maiti, Balamurali M M, Kaushik Chanda
The aim of this patent evaluation is to point out recent advances made in the field of synthesis of rufinamide which will encourage scientists further to design and develop new synthetic routes to rufinamide. The invention in this patent application relates to the synthesis of rufinamide 1 and its intermediates using activated acetylenic esters as dipolarophile for the treatment ofLGS. At present most of the synthetic methods for the synthesis of rufinamide involved the use of costly 2-chloroacrylonitrile, propiolic acid, and esters which is time consuming, low yields and often coupled with the problem of regioselectivity. In an effort to attain the regioselective synthesis of rufinamide, several Cu(I) catalyzed synthetic routes have been developed. In this patent evaluation, a large number of activated acetylenic esters were prepared from N-hydroxy succinimide, N-hydroxyphthalimide, 1-hydroxy benzotriazole, or 4-nitro phenol. Further the acetylenic esters were investigated for Cu(I) catalyzed 1,3-dipolar cycloaddition reaction to obtain the rufinamide in good yields. Further the patent also synthesized the rufinamide through in-situ generated activated acetylenic esters in one-pot methodology which saves the time and provided efficient yields. This patent provides good examples of using activated acetylenic esters as dipolarophile for the synthesis of rufinamide using regioselective Cu catalyzed cycloaddtion of dipolarophiles with 2,6-difluro benzyl azide in three steps. These activated acetylenic esters may be good lead for the discovery of more potent anitiepileptic drugs for the treatment of neurological disorder. The synthesized activated acetylenic esters are regarded as useful synthons. Moreover, these activated acetylenic esters can be useful for amide and ester synthesis with amines or alcohols, acylation reactions, and five-member heterocyclic molecule syntheses.