3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 2: Optimization of the side chains to improve in vitro and in vivo potencies

International Union of Basic and Clinical Pharmacology. LXXXIII: Classification of Prostanoid Receptors, Updating 15 Years of Progress

“…An EP 3 antagonist of a different class is represented by compound 49 (Fig. 5) (Asada et al, 2010); it showed good in vivo activity against PGE 2 -induced contraction of pregnant rat uterus.…”

Enantioselective Decarboxylative Arylation of α-Amino Acids via the Merger of Photoredox and Nickel Catalysis

“…To highlight the utility of this asymmetric cross-coupling reaction, we applied our protocol to the synthesis of the cores of pharmacologically active molecules. Using the conditions outlined in Table , N -Boc-leucine was successfully cross-coupled to provide protected benzylic amines 7 and 8 in good yield and excellent enantioselectivity (Scheme ). Products 7 , bearing bis-trifluoro­methyl­phenyl substitution, and 8 , bearing a methylbenzoate group, could be advanced to the corresponding bioactive compounds through straightforward synthetic sequences (e.g., amide coupling and Buchwald–Hartwig amination).…”

Ru-Catalyzed Asymmetric Addition of Arylboronic Acids to Aliphatic Aldehydes via P-Chiral Monophosphorous Ligands

“…1-(4-chlorophenyl)-3-methylbutan-1-ol (3fe) [97] [a] 20 D = +37.9 (c 0.81, CH 2 Cl 2 ). Yield: 82% (81.4 mg) as a light-yellow oil; 1 H NMR (400 MHz, CDCl 3 ) δ 7.27 (q, J = 8.5, 4H), 4.69 (dd, J = 8.1, 5.3, 1H), 2.08 (s, 1H), 1.73-1.57 (m, 2H), 1.50-1.38 (m, 1H) and 0.93 (dd, J = 6.4, 2.0, 6H).…”