219727-44-3Relevant academic research and scientific papers
INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
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Page/Page column 34, (2013/05/21)
The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir 1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
Preparation of new polyfunctional magnesiated heterocycles using a chlorine-, bromine-, or iodine-magnesium exchange
Abarbri, Mohamed,Thibonnet, Jerome,Berillon, Laurent,Dehmel, Florian,Rottlaender, Mario,Knochel, Paul
, p. 4618 - 4634 (2007/10/03)
The reaction of heteroaryl iodides with i-PrMgBr (ca. 1.0 equiv) in THF provides the corresponding magnesiated heterocycles. Functional groups such as an ester, cyano, or chloride functions are tolerated in these new Grignard reagents if the exchange can be performed below -20 °C. This is the case for all heterocycles bearing electron-withdrawing groups or chelating functions facilitating the iodine-magnesium exchange. In many cases, the exchange can be extended to heteroaryl bromides, and a case of a chlorine-magnesium exchange is described with tetrachlorothiophene. This new preparation of functionalized heteroarylmagnesium compounds provides after reaction with various electrophiles a new entry to a broad range of polyfunctional pyridines, imidazoles, furanes, thiophenes, pyrroles, antipyrines, and uracil derivatives. The application of the halogenmagnesium exchange in the solid phase allows the performance of solid-phase synthesis, with potential applications for combinatorial chemistry.
Preparation of highly functionalized pyridylmagnesium reagents for the synthesis of polyfunctional pyridines
Bérillon, Laurent,Leprêtre, Anne,Turck, Alain,Plé, Nelly,Quéguiner, Guy,Cahiez, Gérard,Knochel, Paul
, p. 1359 - 1360 (2007/10/03)
Functionalized iodopyridines bearing either a chloride, ester or nitrile function were converted to the corresponding organomagnesium derivatives at -40°C or -78°C by treatment with i-PrMgBr (1.1 equiv, 0.5 h, > 90% yield). The resulting functionalized Grignard reagents react with aldehydes, TosCN directly or with allylic bromides and benzoyl chloride after transmetalation with CuCN leading to polyfunctional pyridines.
