100360-56-3Relevant academic research and scientific papers
AN IMPROVED PROCESS FOR THE PREPARATION OF (1S, 4S, 7Z, 10S, 16E, 21R)- 7-ETHYLIDENE-4,21-BIS(1-METHYLETHYL)-2-OXA-12,13-DITHIA-5, 8, 20, 23- TETRAAZABICYCLO[8.7.6]TRICOS-16-ENE-3, 6, 9, 19, 22-PENTONE
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Page/Page column 26, (2017/05/19)
The present invention is relates to an improved process for the preparation (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-bis(1-methylethyl)-2-oxa-12,13-dithia-5,8,20,23-tetraazabi-cyclo[8.7.6]tricos-16-ene-3,6,9,19,22-pentone of formula I.
A method for preparing derivatives of folic acid Hydrosulfuryl
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Paragraph 0041-0043, (2016/12/01)
The invention discloses a preparation method of a folic acid sulfhydrylation derivative. The preparation method comprises the following steps that -SH in thiol is protected to obtain a derivative of thiol, so that sulfydryl having high reaction activity is protected; then, in the presence of a catalyst and a dehydrating agent, esterification reaction is carried out between hydroxyl on the protected thiol derivative and folic acid, so that a modified folic acid derivative is obtained; a carbon sulphur bond in the folic acid derivative is broken through reduction reaction; sulfydryl is formed again in a product, and therefore, the target product, namely sulfhydrylation folic acid, is obtained. According to the preparation method disclosed by the invention, trityl chloride is replaced by triphenylcarbinol; the disadvantages of difficulty in separation of products and lower product yield are overcome; the product yield is increased; in the esterification reaction, a solid catalyst (macroporous cation exchange resin) is adopted, so that the separation efficiency of products is greatly improved; micromolecules, such as 4-dimethylamino-pyridine (DMAP), are adopted in normal biological preparation; the micromolecules are easily dissolved in a solvent and difficult to separate.
Peptide ligation assisted by an auxiliary attached to amidyl nitrogen
Li, Juan,Cui, Hong-Kui,Liu, Lei
scheme or table, p. 1793 - 1796 (2010/06/13)
New thiol-containing auxiliaries were developed for peptide ligation. They were placed at the amidyl N-atom in the second amino acid residue of a peptide fragment. With the new auxiliaries, peptide ligation could be conducted at non-Cys and non-Gly sites. Compared to other recently developed auxiliaries, an important feature of the present design was that the new auxiliaries were generally applicable and readily removable.
Synthesis of pyridine-based polyaminocarboxylic ligands bearing a thioalkyl anchor
Lin, Yi,Favre-Réguillon, Alain,Pellet-Rostaing, Stéphane,Lemaire, Marc
, p. 3463 - 3466 (2008/02/10)
A bicyclic tetraazatriacetic chelating agent containing a thioalkyl pendant group was prepared. Four synthetic routes have been investigated via a Mitsunobu reaction from 2,4-[bishydroxymethyl]-3-hydroxy-pyridine 1. Deprotection of trityl thioether compound 5c led to ligand 6c in 22% overall yield from the starting 3-hydroxypyridine.
INHIBITOR IMAGING AGENTS
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Page/Page column 49, (2010/02/12)
The present invention discloses that imaging agents which comprise a specific type of matrix metalloproteinase inhibitors (MMPi's) of the sulphonamide hydroxamate class labelled with an imaging moiety, are useful diagnostic imaging agents for in vivo imag
