381665-66-3Relevant academic research and scientific papers
5-MEMBERED HETEROARYLAMINOSULFONAMIDES FOR TREATING CONDITIONS MEDIATED BY DEFICIENT CFTR ACTIVITY
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Page/Page column 418; 419, (2021/05/21)
The invention relates to heteroaryl compounds, pharmaceutically acceptable salts thereof, and pharmaceutical preparations thereof. Also described herein are compositions and the use of such compounds in methods of treating diseases and conditions mediated by deficient CFTR activity, in particular cystic fibrosis.
Design and synthesis of 4-substituted benzamides as potent, selective, and orally bioavailable IKs blockers
Lloyd,Schmidt,Rovnyak,Ahmad,Atwal,Bisaha,Doweyko,Stein,Traeger,Mathur,Conder,DiMarco,Harper,Jenkins-West,Levesque,Normandin,Russell,Serafino,Smith,Lodge
, p. 3764 - 3767 (2007/10/03)
Multiple delayed rectifier potassium currents, including IKs, are responsible for the repolarization and termination of the cardiac action potential, and blockers of these currents may be useful as antiarrhythmic agents. Modification of compound 5 produced 19(S) that is the most potent IKs blocker reported to date with > 5000-fold selectivity over other cardiac ion channels. Further modification produced 24A with 23% oral bioavailability.
Asymmetric nitroalkene [4 + 2] cycloadditions: Enantioselective synthesis of 3-substituted and 3,4-disubstituted pyrrolidines
Denmark,Marcin
, p. 3221 - 3235 (2007/10/02)
2-Substituted 1-nitroalkenes undergo highly diastereoselective, Lewis-acid-promoted, [4 + 2] cycloaddition with chiral vinyl ethers derived from (R)-2,2-diphenylcyclopentanol and (1R,2S)-2-phenylcyclohexanol to afford cyclic nitronates in high yields. The resulting nitronates were reduced with hydrogen at 160 psi in the presence of platinum oxide to afford enantiomerically enriched pyrrolidines (both as the free base and N-protected derivatives) in good yields. A series of 3-substituted pyrrolidines (71-97% ee) were prepared, as well as (3S,4R)-4-methyl-3-phenyl-N-(p-tolylsulfonyl)pyrrolidine (92% ee) and (3S,4S)-3,4-diphenylpyrrolidine (99% ee). The chiral auxiliaries can be recovered in nearly quantitative yields after hydrogenation.
