All about Drugs Live by Dr Anthony Melvin Crasto
1-(4-fluorophenyl)-6-methyl-2-oxo-1,2-dihydropyridine-3-carboxylic pivalic anhydride (10): tan solid, mp (DSC): onset = 172.4 °C, peak temperature = 173.0 °C; 1H NMR (400 MHz, CD3CN) δ 8.23 (d, J = 7.6 Hz, 1 H), 7.35–7.25 (m, 4 H), 6.36 (d, J = 8.0 Hz, 1 H), 2.02 (s, 3 H), 1.25 (s, 9 H); 13C NMR (100 …
Efforts toward route evaluation and process optimization for the preparation of brexpiprazole (1) are described. Starting from commercially available dihydroquinolinone 11, a three-step synthesis route composed of O-alkylation, oxidation, and N-alkylation was selected for industry-oriented process development aiming to reduce side reactions and achieve better impurity profiles. The reaction conditions of the three steps were investigated, and the …
A practical and scalable synthetic method to obtain dolutegravir sodium (1) was established starting from the readily accessible material maltol (2). This synthetic method includes a scalable oxidation process of maltol and palladium-catalyzed amidation for introduction of an amide moiety, leading to a practical manufacturing method in short synthetic steps. The synthetic method demonstrated herein …
2,4-Diphenyl-2,3-dihydro-1,5-benzothiazepine (4a) 1,3-Diphenyl-2-propen-1-one (1a). Yellow solid; mp 114-116 C [lit.1 , 114-115 °C], AcOEt/PE 1:9. 1H NMR (300 MHz, CDCl3,): 3.07 (t, J = 12.6 Hz, 1 H), 3.32 (dd, J = 4.7, 13.1 Hz, 1 H), 4.99 (dd, J = 4.5, 12.0 Hz, 1 H), 7.12-7.17 (m, 1 H), 7.25-7.30 (m, 5 H), 7.44-7.51 …
Cross dehydrogenative coupling of N-aryltetrahydroisoquinolines (sp3 C-H) with indoles (sp2 C-H) using a heterogeneous mesoporous manganese oxide catalyst Green Chem., 2017, Advance Article DOI: 10.1039/C7GC01919J, Communication B. Dutta, V. Sharma, N. Sassu, Y. Dang, C. Weerakkody, J. Macharia, R. Miao, A. R. Howell, S. L. Suib We disclose a novel, heterogeneous catalytic approach for selective …
Trelagliptin succinate, a novel once-weekly oral dipeptidyl peptidase-4 (DPP-4) inhibitor, was approved for the Japanese market on March 26, 2015 Trelagliptin exhibited a better potency against human DPP-4 than alogliptin and sitagliptin, along with its excellent selectivity and slow-binding properties that may partially contribute to its sustained efficacy. In phase III clinical studies, once-weekly oral trelagliptin …
Regioselective access of alkylidendibenzo[c,f]oxocine framework via cyclocarbopalladation/cross-coupling cascade reactions and reductive Heck strategy New J. Chem., 2017, Advance Article DOI: 10.1039/C6NJ03825E, Paper Tapas Ghosha a Institute of Organic Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany E-mail: tapas.ghosh@uni-wuerzburg.de,tapasghosh.chem@gmail.com Tel: +49-931-31-81629 New J. Chem., 2017, Advance Article DOI: 10.1039/C6NJ03825E Palladium-catalyzed dual strategies of cascade cyclocarbopalladation/cross-coupling …
The use of biodiesel has been promoted for the past decade as a substitute for fossil-based diesel fuel. However, it has become evident that its production competes with food production by engrossing cropland. To overcome this Corma has developed a process that uses 2-methylfuran which currently is isolated (280 × 103 tonnes per year) from …
Continuous flow Doebner–Miller synthesis of different quinaldines from respective anilines is demonstrated using sulfuric acid as a homogeneous catalyst. The extent of reaction was monitored for various parameters, namely, temperature, residence time, mole ratio of sulfuric acid to substrate, mole ratio of crotonaldehyde to substrate, and so forth. Continuous stirred reactors in series were used …