2(1H)-Quinolinone derivatives as novel anti-arteriostenotic agents showing anti-thrombotic and anti-hyperplastic activities

Process Development on the Preparation of trans-(+)-2-Methylaminocyclohexanol: A Fascinating Resolution Example

“…Single isomers of trans -(±)-2-methylaminocyclohexanol [(+)-MAC and (−)-MAC] are important intermediates for the preparation of nitrogen-containing cycloalkylaminoaryl derivatives for CNS disorder,1b analgesia agents,1c and anti-arteriostenotic agents 1a. They are also important chiral intermediates useful as ligands, chiral auxiliaries, or in other asymmetric synthetic applications .…”

Palladium-Catalyzed Carbonylative Synthesis of Six-Membered Heterocycles from Aryl Halides

“…Quinolinone and its derivatives have diverse chemical and pharmacological properties and thus attracted much interest of both synthetic and pharmaceutical chemists [48][49][50][51][52][53] (Fig. 4).…”

Asymmetric Amination of meso-Epoxide with Vegetable Powder as a Low-Toxicity Catalyst

“…Chiral β-aminoalcohol units are found in many bioactive compounds used for the therapeutic treatment of various diseases [ 1 , 2 , 3 ]. Chiral trans -β-aminocyclohexanol derivatives are particularly useful substrates as key intermediates for the synthesis of 1-cyclopropyl-1-((1 R ,2 R )-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea, which is a phosphodiesterase III inhibitor with vascular hypertrophy effects, and ( R )-1-((1 R ,2 R )-2-(3,4-dimethoxyphenethoxy)cyclohexyl)-pyrrolidin-3-ol, which is an antiarrhythmic agent ( Figure 1 ) [ 4 , 5 , 6 ]. The most effective method to synthesize chiral trans -β-aminocycloalkanols is the catalytic asymmetric amination of the corresponding 1,2-epoxycycloalkanes.…”