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A highly efficient Suzuki-Miyaura methylation of pyridines leading to the drug pirfenidone and its CD3 version (SD-560)

A highly efficient Suzuki-Miyaura methylation of pyridines leading to the drug pirfenidone and its CD3 version (SD-560) Green Chem., 2017, Advance Article DOI: 10.1039/C7GC01740E, Communication Eliezer Falb, Konstantin Ulanenko, Andrey Tor, Ronen Gottesfeld, Michal Weitman, Michal Afri, Hugo Gottlieb, Alfred Hassner The first methylation/deuteromethylation in green and nearly quantitative Suzuki-Miyaura routes to pirfenidone and …

1,2-Bis(3-methoxyphenyl)benzene

1,2-Bis(3-methoxyphenyl)benzene (5) 1H NMR (500 MHz, DMSO-d6): δ 3.59 (s, 6H), 6.65 (dd, J = 2.5, 1.5 Hz, 2H), 6.70 (ddd, J = 7.5, 1.5, 1.0 Hz, 2H), 6.78 (ddd, J= 8.0, 2.5, 1.0 Hz, 2H), 7.16 (t, J = 8.0 Hz, 2H), 7.40–7.46 (m, 4H). 13C NMR (126 MHz, DMSO-d6): δ 54.8, 112.4, 115.0, 121.7, 127.7, 129.0, 130.2, 139.8, 142.4, 158.7. …

Development of a General Protocol To Prepare 2H-1,3-Benzoxazine Derivatives

2H-1,3-Benzoxazine natural products and related bioactive molecules. 4-(2-Bromo-5-chlorobenzyl)-7-chloro-2-phenyl-2H-benzo[e][1,3]oxazine 2 as a light-yellow solid (82% yield). 1H NMR (500 MHz, CDCl3): δ (ppm) 7.55–7.52 (m, 3H), 7.42–7.34 (m, 3H), 7.30 (d, 1H, J = 3.5 Hz,) 7.29 (s, 1H), 7.12 (dd, 1H, J = 8.5 Hz, 2.5 Hz), 6.95–6.91 (m, 2H), 6.57 (1H, s), 4.16 (ABq, 2H, ΔδAB = 0.05, JAB = 16.5 Hz). …

Xanomeline (LY-246,708; Lumeron, Memcor) ксаномелин , كسانوميلين , 诺美林 ,

Xanomeline (LY-246,708; Lumeron, Memcor) CAS 131986-45-3 Molecular FormulaC14H23N3OS Average mass281.417 Da ксаномелин , كسانوميلين , 诺美林 , Hexyloxy-TZTP 5-[4-(Hexyloxy)-1,2,5-thiadiazol-3-yl]-1-méthyl-1,2,3,6-tétrahydropyridine Xanomeline(LY246708) is a selective M1 muscarinic receptor agonist. Pyridine, 3-[4-(hexyloxy)-1,2,5-thiadiazol-3-yl]-1,2,5,6-tetrahydro-1-methyl- Xanomeline(LY246708) is a selective M1 muscarinic receptor agonist. in vitro: Xanomeline had high affinity for muscarinic receptors in brain homogenates, but had substantially less or no affinity for a number of other neurotransmitter receptors and …

Diethyl Chlorophosphate

Diethyl Chlorophosphate (CAS no 814–49–3)(15) Preparative Procedure In a dry four-neck 250 mL round-bottom flask equipped with a mechanical stirrer, a thermometer, and an argon inlet were introduced at 20 °C triethylamine (21.3 g, 210 mmol), tert-butyl methyl ether (75 mL), and ethanol (9.67 g, 210 mmol). Phosphorus oxychloride (15.3 g, 100 mmol) was added …

CARMUSTINE

CARMUSTINE Molecular Formula: C5H9Cl2N3O2 Molecular Weight: 214.046 g/mol CAS 154-93-8 Brain tumor; Hodgkins disease; Multiple myeloma; Non-Hodgkin lymphoma 1,3-bis(2-chloroethyl)-3-nitrosourea Urea, 1,3-bis(2-chloroethyl)-1-nitroso- (8CI) N,N’-Bis(2-chloroethyl)-N-nitrosourea 1,3-Bis(2-chlorethyl)-1-nitrosourea 1,3-Bis(2-chloroethyl)-1-nitrosourea 1,3-Bis(2-chloroethyl)nitrosourea 1,3-Bis(β-chloroethyl)-1-nitrosourea BCNU Becenun BiCNU Carmubris Carmustin Carmustine DTI 015 FDA 0345 Gliadel Gliadel Wafer NSC 409962 Nitrumon SK 27702 SRI 1720 Title: Carmustine CAS Registry Number: 154-93-8 CAS Name: N,N¢-Bis(2-chloroethyl)-N-nitrosourea Additional Names: BCNU Manufacturers’ …

Funapide, TV 45070, XEN-402, фунапид فونابيد 呋纳匹特

Funapide TV 45070, XEN-402, Funapide, (+)- фунапид فونابيد 呋纳匹特 Molecular FormulaC22H14F3NO5 Average mass429.345 Da (S)-1′-[(5-Methyl-2-furyl)methyl]spiro[6H-furo[3,2-f][1,3]benzodioxole-7,3′-indoline]-2′-one Spiro(furo(2,3-F)-1,3-benzodioxole-7(6H),3′-(3H)indol)-2′(1’H)-one, 1′-((5-(trifluoromethyl)-2-furanyl)methyl)-, (3’S)- (3’S)-1′-((5-(Trifluoromethyl)furan-2-yl)methyl)-2H,6H-spiro(furo(2,3-F)(1,3)benzodioxole-7,3′-indol)-2′(1’H)-one Spiro[furo[2,3-f]-1,3-benzodioxole-7(6H),3′-[3H]indol]-2′(1’H)-one, 1′-[[5-(trifluoromethyl)-2-furanyl]methyl]-, (7S)- TV-45070 UNII-A5595LHJ2L XEN-401-S XEN402 (3’S)-1′-{[5-(trifluoromethyl)furan-2-yl]methyl}-2H-6H-spiro[furo[2,3-f]-1,3-benzodioxole-7,3′-indol]-2′(1’H)-one (7S)-1′-{[5-(Trifluoromethyl)-2-furyl]methyl}spiro[furo[2,3-f][1,3]benzodioxole-7,3′-indol]-2′(1’H)-one 1259933-16-8 CAS UNII-A5595LHJ2L Phase II clinical trials for Postherpetic neuralgia (PHN) Treatment of Neuropathic Pain Originator Xenon Pharmaceuticals Developer Teva Pharmaceutical Industries; Xenon Pharmaceuticals Class Benzodioxoles; Fluorobenzenes; Furans; Indoles; Non-opioid analgesics; Small …

Riamilovir, Triazavirin

Riamilovir, Triazavirin Riamilovir sodium dihydrate, CAS 928659-17-0, Riamilovir CAS: 123606-06-4 Chemical Formula: C5H4N6O3S Molecular Weight: 228.19 [1,2,4]Triazolo[5,1-c][1,2,4]triazin-4(1H)-one, 7-(methylthio)-3-nitro- (9CI) 7-(Methylthio)-3-nitro[1,2,4]triazolo[5,1-c][1,2,4]triazin-4(6H)-one 1,2,4]Triazolo[5,1-c][1,2,4]triazin-4(6H)-one, 7-(methylthio)-3-nitro- 7-(methylsulfanyl)-3-nitro[1,2,4]triazolo[5,1-c][1,2,4]triazin- 4(1H)-one 7-thio-substituted-3-nitro-1,2,4-triazolo[5,1-c]-1,2,4-triazin-4(1H)-one Riamilovir sodium CAS 116061-59-7 Riamilovir sodium dihydrate, CAS 928659-17-0, Triazavirin Flavivirus infection; Zika virus infection Zika virus Flavivirus Anti-viral drug http://apps.who.int/medicinedocs/documents/s23256en/s23256en.pdf Triazavirin (TZV) is a broad-spectrum antiviral drug developed in Russia through a joint effort of Ural …

Lifitegrast

Lifitegrast, SAR 1118 SAR-1118-023 CAS 1025967-78-5 Xiidra (lifitegrast ophthalmic solution) FDA approves new medication for dry eye disease 07/12/2016 08:48 AM EDT The U.S. Food and Drug Administration approved Xiidra (lifitegrast ophthalmic solution) for the treatment of signs and symptoms of dry eye disease, on Monday, July 11, 2016. Xiidra is the first medication in …

Vaborbactam, Ваборбактам , فابورباكتام , 法硼巴坦 ,

Vaborbactam RN: 1360457-46-0 UNII: 1C75676F8V Molecular Formula. C12-H16-B-N-O5-S Molecular Weight. 297.1374 1,2-Oxaborinane-6-acetic acid, 2-hydroxy-3-((2-(2-thienyl)acetyl)amino)-, (3R,6S)- B1([C@H](CC[C@H](O1)CC(=O)O)NC(=O)Cc2cccs2)O RPX7009 A beta-lactamase inhibitor. Treatment of Bacterial Infection {(3R,6S)-2-Hydroxy-3-[(2-thienylacetyl)amino]-1,2-oxaborinan-6-yl}acetic acid 2-[(3R,6S)-2-hydroxy-3-[(2-thiophen-2-ylacetyl)amino]oxaborinan-6-yl]acetic acid 1,2-Oxaborinane-6-acetic acid, 2-hydroxy-3-[[2-(2-thienyl)acetyl]amino]-, (3R,6S)- Ваборбактам [Russian] فابورباكتام [Arabic] 法硼巴坦 [Chinese] Originator Rempex Pharmaceuticals Developer The Medicines Company; US Department of Health and Human Services Class Antibacterials; Pyrrolidines; Small molecules; Thienamycins Mechanism of Action Beta lactamase inhibitors; Cell …