Drug Approvals International – Page 126 – All about Drugs Live by Dr Anthony Melvin Crasto

Synthesis, characterization and anti-inflammatory evaluation of novel substituted tetrazolodiazepine derivatives

SRM University Department of Chemistry Chennai, Tamil Nadu, India 3b R = NITRO http://nopr.niscair.res.in/handle/123456789/42358 Dr. S. Sathishkumar Assistant Professor in Chemistry, Kongu Engineering College, Perundurai, Erode – 638052 DR. HELEN P. KAVITHA Dr. Helen P. Kavitha Professor and Head of the Department E-mail: helen.p@rmp.srmuniv.ac.in Area: Chemistry Affiliation: Department of Chemistry, Ramapuram Campus, SRM University Education Ph.D. Organic Synthesis …

Benzo[d]oxazol-2(3H)-one

IH NMR ABOVE 13C NMR BELOW Benzo[d]oxazol-2(3H)-one (2a) pale yellow crystals; mp 140.5–141.5 °C (lit.(6a) 134–136 °C); 1H NMR (300 MHz, CDCl3) δ 9.90 (s, 1H), 7.26–7.09 (m, 4H); 13C NMR (75 MHz, CDCl3) δ 156.3, 143.9, 129.4, 124.2, 122.8, 110.3, 110.2. NMR PREDICT 1H NMR PREDICT 13C NMR PREDICT ////////// http://pubs.acs.org/doi/full/10.1021/acs.oprd.7b00217

LOXO 195

LOXO-195 CAS: 2097002-61-2 Chemical Formula: C20H21FN6O Molecular Weight: 380.4274 2097002-59-8 (RS-isomer) 1350884-56-8 (R racemic) Synonym: LOXO-195; LOXO 195; LOXO195. IUPAC: (13E,14E,22R,6R)-35-fluoro-6-methyl-7-aza-1(5,3)-pyrazolo[1,5-a]pyrimidina-3(3,2)-pyridina-2(1,2)-pyrrolidinacyclooctaphan-8-one 10H-5,7-Ethenopyrazolo[3,4-d]pyrido[2,3-k]pyrrolo[2,1-m][1,3,7]triazacyclotridecin-10-one, 17-fluoro-1,2,3,11,12,13,14,18b-octahydro-12-methyl-, (12R,18bR)- SMILES Code: FC1=CN=C(CC[C@@H](C)NC(C2=C3N(C=CC4=N3)N=C2)=O)C([C@@H]5N4CCC5)=C1 LOXO-195 is a potent and selective TRK inhibitor capable of addressing potential mechanisms of acquired resistance that may emerge in patients receiving larotrectinib (LOXO-101) or multikinase inhibitors with anti-TRK activity. …

NaBH4, twin screw technology (i.e., granulator, melt extruder, etc.) to yield the desired product in a continuous manner

In this work the application of green chemistry principles such as process intensification and the replacement of reagents and solvents to more benign alternatives were coupled with the advantages of continuous manufacturing. The reduction of lipophilic aromatic aldehydes using an aqueous alkaline solution of NaBH4 was achieved by means of mechanical shearing and kneading provided …

Ascaridole

Scheme 2. Photo-Oxidation of α-terpinene 1 to Ascaridole 2 and the Common Byproduct p-Cymene 3 Continuous Photo-Oxidation in a Vortex Reactor: Efficient Operations Using Air Drawn from the Laboratory Darren S. Lee† , Zacharias Amara†, Charlotte A. Clark†, Zeyuan Xu‡, Bruce Kakimpa‡, Herve P. Morvan‡, Stephen J. Pickering‡, Martyn Poliakoff*†, and Michael W. George*†§ †School of Chemistry, ‡Department of Mechanical, Materials and Manufacturing Engineering, University of Nottingham, University Park, Nottingham, NG7 …

Atom- and step-economical nucleophilic arylation of azaaromatics via electrochemical oxidative cross C-C coupling reactions

Atom- and step-economical nucleophilic arylation of azaaromatics via electrochemical oxidative cross C-C coupling reactions Green Chem., 2017, 19,2931-2935 DOI: 10.1039/C7GC00789B, Communication O. N. Chupakhin, A. V. Shchepochkin, V. N. Charushin A simple and efficient electrochemical method for the synthesis of asymmetrical bi(het)aryls through direct functionalization of the C(sp2)-H bond in azaaromatics with fragments of (hetero)aromatic …

Increasing global access to the high-volume HIV drug nevirapine through process intensification

Increasing global access to the high-volume HIV drug nevirapine through process intensification Green Chem., 2017, 19,2986-2991 DOI: 10.1039/C7GC00937B, Paper Jenson Verghese, Caleb J. Kong, Daniel Rivalti, Eric C. Yu, Rudy Krack, Jesus Alcazar, Julie B. Manley, D. Tyler McQuade, Saeed Ahmad, Katherine Belecki, B. Frank Gupton Fundamental elements of process intensification were applied to generate …

Cp2TiCl: An Ideal Reagent for Green Chemistry?

The development of Green Chemistry inevitably involves the development of green reagents. In this review, we highlight that Cp2TiCl is a reagent widely used in radical and organometallic chemistry, which shows, if not all, at least some of the 12 principles summarized for Green Chemistry, such as waste minimization, catalysis, safer solvents, toxicity, …

One-pot synthesis of 2-hydroxymethyl-5-methylpyrazine from renewable 1,3-dihydroxyacetone

One-pot synthesis of 2-hydroxymethyl-5-methylpyrazine from renewable 1,3-dihydroxyacetone Green Chem., 2017, Advance Article DOI: 10.1039/C7GC00578D, Communication Lei Song, Mingyuan Zheng, Jifeng Pang, Joby Sebastian, Wentao Wang, Minjie Qu, Jian Zhao, Xinhong Wang, Tao Zhang An efficient and environmentally benign method for the synthesis of 2-hydroxymethyl-5-methylpyrazine (HMMP) from biomass derived 1,3-dihydroxyacetone was developed. From the journal: …

Imigliptin dihydrochloride, Xuanzhu Pharma Co Ltd, NEW PATENT, WO 2017107945

Imigliptin dihydrochloride, Xuanzhu Pharma Co Ltd, NEW PATENT, WO 2017107945 https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2017107945&redirectedID=true Applicants: XUANZHU PHARMA CO.,LTD. [CN/CN]; 2518, Tianchen Street, National High-tech Development Zone Jinan, Shandong 250101 (CN) Inventors: SHU, Chutian; (CN). WANG, Zhenhua; (CN) The present invention relates to a crystalline form of benzoate of a dipeptidyl peptidase-IV inhibitor, a method for preparing the same, a pharmaceutical composition,and …