30186-24-4Relevant articles and documents
PHD INHIBITOR COMPOUNDS, COMPOSITIONS, AND USE
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Paragraph 0355-0356, (2021/09/26)
The present invention provides, in part, novel small molecule inhibitors of PHD, having a structure according to Formula (A), and sub-formulas thereof: or a pharmaceutically acceptable salt thereof. The compounds provided herein can be useful for treatment of diseases including heart ( e.g. ischemic heart disease, congestive heart failure, and valvular heart disease), lung (e.g., acute lung injury, pulmonary hypertension, pulmonary fibrosis, and chronic obstructive pulmonary disease), liver (e.g. acute liver failure and liver fibrosis and cirrhosis), and kidney (e.g. acute kidney injury and chronic kidney disease) disease.
Metal-free arylation of ethyl acetoacetate with hypervalent diaryliodonium salts: An immediate access to diverse 3-aryl-4(1 H)-quinolones
Monastyrskyi, Andrii,Namelikonda, Niranjan K.,Manetsch, Roman
, p. 2513 - 2520 (2015/03/18)
A clean arylation protocol of ethyl acetoacetate was developed using hypervalent diaryliodonium salts under mild and metal-free conditions. The scope of the reaction, using symmetric and unsymmetric iodonium salts with varying sterics and electronics, was examined. Further, this method has been applied for the synthesis of antimalarial compound ELQ-300, which is currently in preclinical development.
Regiospecific Homologation of Unsymmetrical Ketones
Dave, Vinod,Warnhoff, E. W.
, p. 2590 - 2598 (2007/10/02)
A method has been developed for the regiospecific homologation of unhindered unsymmetrical ketones.The procedure consists of preparation of a pure α-halo ketone, reaction of this derivative with ethyl diazoacetate and boron trifluoride etherate, removal of the halogen by zinc reduction, and finally decarbethoxylation with water at 230 deg C or with CaCl2*2H2O in dimethyl sulfoxide at 150 deg C.The method depends on the electron-withdrawing power of the α-halogen to prevent the migration of the attached carbon.A-Homo steroid ketones are most conveniently prepared by this method.The reaction of α-acetoxy ketones with ethyl diazoacetate also leads mainly to migration of the unsubstituted α'-carbon atom.
