Category «Uncategorized»

Synthesis of tetrazines from gem-difluoroalkenes under aerobic conditions at room temperature

It’s only fair to share… Synthesis of tetrazines from gem-difluoroalkenes under aerobic conditions at room temperature Green Chem., 2017, Advance Article DOI: 10.1039/C6GC03494B, Paper Zheng Fang, Wen-Li Hu, De-Yong Liu, Chu-Yi Yu, Xiang-Guo Hu A procedure for the synthesis of tetrazines from gem-difluoroalkenes under aerobic conditions has been developed. Synthesis of tetrazines from gem-difluoroalkenes under …

Photobiocatalytic alcohol oxidation using LED light sources

It’s only fair to share… Photobiocatalytic alcohol oxidation using LED light sources Oxidative lactonization of meso-3-methyl-1,5-pentanediol to (S)-4-methyltetrahydro-2H-pyran-2-one using horse liver alcohol dehydrogenase (HLADH) and photocatalytic, aerobic regeneration of NAD+. Green Chem., 2017, 19,376-379 DOI: 10.1039/C6GC02008A, Communication Open Access   This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. M. Rauch, S. …

New Patent, (S)-pregabalin, WO 2017019791, Teva

It’s only fair to share… Synthesis of (S)-pregabalin, Teva WO-2017019791 TEVA PHARMACEUTICALS INTERNATIONAL GMBH [CH/CH]; Schusselstrasse 12 8645 Jona (CH) (For All Designated States Except US). JANAGANI, Satyanarayana [US/US]; (US) (US only) Improved process for preparing (S)-pregabalin, useful for treating pain, seizures, convulsions and anxiety. Also claims novel intermediates of (S)-pregabalin and their preparation method. …

1 (4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-4-ol)

It’s only fair to share… 1 (4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-4-ol) Examples Example 1 – Preparation Of Compound 1 (4-(3-(methylsulfonyl)phenyl)-l-propylpiperidin-4-ol) 4-(3-(methylthio)phenyl)-1 – 4-(3-(methylsulfonyl)phenyl)- propylpiperidin-4-ol 1 -propylpiperidin-4-ol To a suspension of 4-hydroxy-4-(3-(methylthio)phenyl)-l-propylpiperidin-l-ium chloride (140g, 348mmol) in 710mL water were added 1.5g sodium tungstate dihydrate, and the mixture was heated to 45°C. 102mL of 33%H202 were added in 20min at 45-55°C. …

Hoshinolactam, A new antitrypanosomal lactam

It’s only fair to share…   Tropical diseases caused by parasitic protozoa are a threat to human health, mainly in developing countries. Trypanosomiasis (Chagas disease and sleeping sickness) and leishmaniasis, inter alia, are classified as neglected tropical diseases, and over 400 million people are at risk of contracting these diseases. In addition, a parasite of …

AMG-3969

It’s only fair to share… AMG-3969 M.Wt: 522.46 Cas : 1361224-53-4 , MF: C21H20F6N4O3S WO 2012027261 PRODUCT PATENT Inventors Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, Jean …

Pridopidine

It’s only fair to share… Pridopidine Molecular Formula C15H23NO2S Average mass 281.414 Da 346688-38-8  CAS FREE FORM 882737-42-0 (hydrochloride) 1440284-30-9 HBr 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidin 4- (3 -Methanesulfonyl-phenyl ) – 1-propyl -piperidine ACR16 Huntexil UNII-HD4TW8S2VK; 4-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine ACR 16 ASP 2314 FR 310826 Huntingtons chorea Dopamine D2 receptor antagonist; Opioid receptor sigma agonist 1 Neurosearch INNOVATORS, In 2012, the product was acquired by …

BMS-960

It’s only fair to share… BMS-960 PRECLINICAL (S)-1-((S)-2-Hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)piperidine-3-carboxylic Acid 3-Piperidinecarboxylic acid, 1-[(2S)-2-hydroxy-2-[4-[5-[3-phenyl-4-(trifluoromethyl)-5-isoxazolyl]-1,2,4-oxadiazol-3-yl]phenyl]ethyl]-, (3S)- (S)-1-((S)-2-Hydroxy-2-(4-(5-(3-phenyl-4-(trifluoromethyl)isoxazol-5-yl)-1,2,4-oxadiazol-3-yl)phenyl)ethyl)piperidine-3-carboxylic Acid CAS 1265321-86-5 FREE FORM FREE FORM 528.48, C26 H23 F3 N4 O5 CAS 1265323-40-7 HCL SALT BASIC PATENT WO201117578, 2011, (US Patent 8399451) Inventors John L. Gilmore, James E. Sheppeck Applicant Bristol-Myers Squibb Company   Sphingosine-1-phosphate (S1P) is the endogenous ligand for the …

Plinabulin

It’s only fair to share… Plinabulin Molecular FormulaC19H20N4O2 Average mass336.388 Da (3Z,6Z)-3-Benzylidène-6-{[4-(2-méthyl-2-propanyl)-1H-imidazol-5-yl]méthylène}-2,5-pipérazinedione 2,5-Piperazinedione, 3-[[5-(1,1-dimethylethyl)-1H-imidazol-4-yl]methylene]-6-(phenylmethylene)-, (3Z,6Z)- CAS 714272-27-2 NPI 2358 NPI-2358; NPI 2358 UNII:986FY7F8XR Phase 3 Clinical Tubulin antagonist Cancer; Febrile neutropenia; Non-small-cell lung cancer Plinabulin (chemical structure, BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and is in a world-wide Phase …