70237-44-4Relevant articles and documents
Scalable and selective deuteration of (hetero)arenes
Bartling, Stephan,Beller, Matthias,Bourriquen, Florian,Brückner, Angelika,Junge, Kathrin,Kreyenschulte, Carsten,Lei, Aiwen,Li, Wu,Lund, Henrik,Rabeah, Jabor,Rockstroh, Nils,Surkus, Annette-Enrica,Yang, Dali
, (2022/01/19)
Isotope labelling, particularly deuteration, is an important tool for the development of new drugs, specifically for identification and quantification of metabolites. For this purpose, many efficient methodologies have been developed that allow for the small-scale synthesis of selectively deuterated compounds. Due to the development of deuterated compounds as active drug ingredients, there is a growing interest in scalable methods for deuteration. The development of methodologies for large-scale deuterium labelling in industrial settings requires technologies that are reliable, robust and scalable. Here we show that a nanostructured iron catalyst, prepared by combining cellulose with abundant iron salts, permits the selective deuteration of (hetero)arenes including anilines, phenols, indoles and other heterocycles, using inexpensive D2O under hydrogen pressure. This methodology represents an easily scalable deuteration (demonstrated by the synthesis of deuterium-containing products on the kilogram scale) and the air- and water-stable catalyst enables efficient labelling in a straightforward manner with high quality control. [Figure not available: see fulltext.].
STEROIDS AND PROTEIN-CONJUGATES THEREOF
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Paragraph 0885-0888, (2018/05/27)
Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells.
Microwave mediated hydrogen deuterium exchange: A rapid synthesis of 2H-substituted benzimidazole
Vaidyanathan, Srirajan,Surber, Bruce W.
, p. 5195 - 5197 (2007/10/03)
Deuterium aromatic substituted compounds were prepared by microwave irradiation of the parent unlabeled compounds in the presence of deuterium oxide and deuterium chloride. The percentage of deuterium incorporation was investigated under various reaction
