Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry

It’s only fair to share…   Advances in indoleamine 2,3-dioxygenase 1 medicinal chemistry Med. Chem. Commun., 2017, 8,1378-1392 DOI: 10.1039/C7MD00109F, Review Article  Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. Alice Coletti, Francesco Antonio Greco, Daniela Dolciami, Emidio Camaioni, Roccaldo Sardella, Maria Teresa Pallotta, Claudia Volpi, Ciriana Orabona, Ursula Grohmann, …

3-Phenylpropionic acid

It’s only fair to share…     3-Phenylpropionic acid (2z) 1 1) Jiang, X.; Zhang, J.; Ma. S. J. Am. Chem. Soc. 2016, 138, 8344 Yield: 94% (142 mg), white solid. Melting point: 47-49 °C (lit.18 49 °C) (18) Helavi, V. B.; Solabannavar, S. B.; Desai, U. V.; Mane, R. B. J. Chem. Research 2003, …

GSK 2330672

It’s only fair to share…   GSK 2330672 GSK 672; GSK-2330672 RN: 1345982-69-5 UNII: 386012Z45S CAS: 1345982-69-5 Chemical Formula: C28H38N2O7S Molecular Weight: 546.68 Pentanedioic acid, 3-((((3R,5R)-3-butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl)methyl)amino)- Pentanedioic acid, 3-((((3R,5R)-3-butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl)methyl)amino)- 3-({[(3R,5R)-3-butyl-3-ethyl-7-(methyloxy)-1 ,1 -dioxido-5-phenyl- 2,3,4,5-tetrahydro-1 ,4-benzothiazepin-8-yl]methyl}amino)pentanedioic acid 3-[[[(3R,5R)-3-Butyl-3-ethyl-2,3,4,5-tetrahydro-7-methoxy-1,1-dioxido-5-phenyl-1,4-benzothiazepin-8-yl]methyl]amino]pentanedioic acid Originator GlaxoSmithKline Class Antihyperglycaemics Mechanism of Action Sodium-bile acid cotransporter-inhibitors Highest Development Phases Phase II Primary biliary cirrhosis; Pruritus; Type 2 diabetes mellitus Phase …

syn-3,5-Dihydroxy Hexanoate

It’s only fair to share…   pure 8 (2.4 g, HPLC purity, 92%). [α]D25 = −41.3 (c = 1.0, CHCl3), >99.5% de.(8g, 9) 1H NMR (CDCl3, 400 MHz), δ/ppm: 1.47 (s, 9H), 1.71–1.75 (m, 2H), 2.42–2.44 (m, 2H), 2.54–2.56 (m, 2H), 3.71 (brs, 2H), 4.18–4.22 (m, 1H), 4.26–4.31 (m, 1H).   t-butyl 6-cyano-(5R)-hydroxy-3-oxo-hexanoate t-Butyl-6-cyano-(3R,5R)-dihydroxyhexanoate is an advanced chiral precursor for the …

(7R, 8S, 8′S, 7″S, 8″R)-abiesol A 4″-O-β-d-glucopyranoside, capselloside.

It’s only fair to share… (7R, 8S, 8′S, 7″S, 8″R)-abiesol A 4″-O-β-d-glucopyranoside, and it was named capselloside. Capselloside (1): Brownish gum; [α]25D −34.0 (c = 0.05, MeOH); UV (MeOH) λmax (log ε) 280 (1.4), 228 (3.3), 214 (3.1) nm; IR (KBr) νmax 3261, 2946, 2816, 1638, 1489, 1261 cm−1; CD (MeOH) λmax (Δ ε) 291 (−), 280 (−) 257 (−) 230 (−) …

GSK 2982772

It’s only fair to share… CAS: 1622848-92-3 (free base),  1987858-31-0 (hydrate) Chemical Formula: C20H19N5O3 Molecular Weight: 377.404 5-Benzyl-N-[(3S)-5-methyl-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepin-3-yl]-4H-1,2,4-triazole-3-carboxamide (S)-5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][l,4]oxazepin-3-yl)-4H-l,2,4- triazole-3-carboxamide 3-(Phenylmethyl)-N-[(3S)-2,3,4,5-tetrahydro-5-methyl-4-oxo-1,5-benzoxazepin-3-yl]-1H-1,2,4-triazole-5-carboxamide (S)-5-Benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide GSK2982772 is a potent and selective receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate for the Treatment of Inflammatory Diseases. GSK2982772 is, currently in phase 2a clinical studies for psoriasis, rheumatoid arthritis, and …

Iron-catalyzed dehydrogenation reactions and their applications in sustainable energy and catalysis

It’s only fair to share…     Iron-catalyzed dehydrogenation reactions and their applications in sustainable energy and catalysis Catal. Sci. Technol., 2017, Advance Article DOI: 10.1039/C7CY00879A, Minireview Ekambaram Balaraman, Avanashiappan Nandakumar, Garima Jaiswal, Manoj K. Sahoo This review article describes recent developments of iron-based acceptorless dehydrogenation (AD) reactions of fundamentally important feedstock, as a route …

Voxilaprevir, فوكسيلابريفير , 伏西瑞韦 , Воксилапревир

It’s only fair to share… Voxilaprevir Molecular FormulaC40H52F4N6O9S Average mass868.934 Da  1535212-07-7 cas (1R,18R,20R,24S,27S,28S)-N-[(1R,2R)-2-(Difluoromethyl)-1-{[(1-methylcyclopropyl)sulfonyl]carbamoyl}cyclopropyl]-28-ethyl-13,13-difluoro-7-methoxy-24-(2-methyl-2-propanyl)-22,25-dioxo-2,21-dioxa-4,11,2  ;3,26-tetraazapentacyclo[24.2.1.03,12.05,10.018,20]nonacosa-3(12),4,6,8,10-pentaene-27-carboxamide Cyclopropanecarboxamide, N-[[[(1R,2R)-2-[5,5-difluoro-5-(3-hydroxy-6-methoxy-2-quinoxalinyl)pentyl]cyclopropyl]oxy]carbonyl]-3-methyl-L-valyl-(3S,4R)-3-ethyl-4-hydroxy-L-prolyl-1-amino-2-(difluoromethyl)-N-[(1-methylcyclopropyl)sulfonyl]-, cyclic (1→2)-ether, (1R,2R)- (laR,5S,8S,9S,10R,22aR)-5-teri-butyl- V-[(lR,2R)-2-(difluoromethyl)– 1-{ [(1-methylcyclopr opyl)sulfonyl] carbamoyl} cyclopropyl] -9-ethyl- 18,18- difluoro-14-methoxy-3,6-dioxo-l,la,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19] [1,10,3,6] dioxadiazacyclononadecino[ll,12-6]quinoxaline-8- carboxamide (laR,5S,8S,9S,10R,22aR)-5-teri-butyl- V-[(lR,2R)-2-(difluoromethyl)- 1-{ [(1-methylcyclopr opyl)sulfonyl] carbamoyl} cyclopropyl] -9-ethyl- 18,18- difluoro-14-methoxy-3,6-dioxo-l,la,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-8H-7,10-methanocyclopropa[18,19] [1,10,3,6] dioxadiazacyclononadecino[ll,12-6]quinoxaline-8- carboxamide 8H-7,10-Methanocyclopropa[18,19][1,10,3,6]dioxadiazacyclononadecino[11,12-b]quinoxaline-8-carboxamide, N-[(1R,2R)-2-(difluoromethyl)-1-[[[(1-methylcyclopropyl)sulfonyl]amino]carbonyl]cyclopropyl]-5-(1 ,1-dimethylethyl)-9-ethyl-18,18-difluoro-1,1a,3,4,5,6,9,10,18,19,20,21,22,22a-tetradecahydro-14-methoxy-3,6-dioxo-, (1aR,5S,8S,9S,10R,22aR)- GS-9857 UNII:0570F37359 Воксилапревир [Russian] [INN] فوكسيلابريفير [Arabic] [INN] 伏西瑞韦 [Chinese] [INN] Voxilaprevir is a hepatitis …

Simple Metal-Free Direct Reductive Amination Using Hydrosilatrane to Form Secondary and Tertiary Amines

It’s only fair to share… Simple Metal-Free Direct Reductive Amination Using Hydrosilatrane to Form Secondary and Tertiary Amines (pages 1872–1878) Sami E. Varjosaari, Vladislav Skrypai, Paolo Suating, Joseph J. M. Hurley, Ashley M. De Lio, Thomas M. Gilbert and Marc J. Adler Version of Record online: 22 MAY 2017 | DOI: 10.1002/adsc.201700079 Simple Metal-Free Direct Reductive …