28781-85-3Relevant academic research and scientific papers
METHOD FOR MANUFACTURING DIFLUOROMETHYLENE COMPOUND
-
Paragraph 0204-0207, (2020/03/28)
The problem to be solved by the present invention is to provide a novel method for producing a difluoromethylene compound. This problem is solved by a method for producing a difluoromethylene compound containing a —CF2— moiety, the method comprising step A of mixing: a) a carbonyl compound containing a —C(O)— moiety;b) optionally an amine;c) a fluoride represented by the formula: MF, wherein M represents a Group 1 element of the periodic table;d) a halogenated fluorine compound represented by the formula: XFn, wherein X represents chlorine, bromine, or iodine, and n is a natural number of 1 to 5; ande) sulfur chloride.
METHOD FOR PREPARING FLUOROORGANIC COMPOUNDS
-
Paragraph 0151; 0152, (2020/08/12)
A process for preparing a compound of formula (I) HR1R2C—CF2—(C═O)—Y starting with a compound of formula (II) R1R2C═CX—(C═O)—Y or of formula (III) HR1R2C—CX1X2—(C═O)—Y placed in contact with hydrofluoric acid; R1 and R2 being independently selected from H, F, Cl, Br, I, C1-C20-alkyl, C6-C20-aryl and C2-C20-alkenyl, C3-C20-cycloalkenyl and C3-C20-cycloalkyl; X1 and X2 being independently selected from F, Cl, Br and I on condition that X1 and X2 are not simultaneously F; Y being selected from the group of H, C1-C20-alkyl, C1-C20-haloalkyl, C6-C20-aryl, —OH, —OR, —NH2, —NHR, —NR2, —SR, C3-C20-cycloalkyl, C3-C20-cycloalkenyl and C2-C20-alkenyl; R being independently selected from the group of C1-C20-alkyl, C6-C20-aryl and C2-C20-alkenyl, C3-C20-cycloalkenyl and C3-C20-cycloalkyl.
Α, α-difluoropropionic production of esters
-
Paragraph 0123-0125, (2016/10/10)
PROBLEM TO BE SOLVED: To provide a practical method of producing α,α-difluoro esters important as pharmaceutical and agricultural chemical intermediates. SOLUTION: The α,α-difluoro esters are produced by reacting α-halogeno-α-fluoro esters with salts or complexes comprising an organic base and hydrogen fluoride. Dehydrohalogenation of side reaction is controlled in the production method. Only α-fluoro-α,β-unsaturated esters of by-products are treated to be brought specifically into a high boiling-point, a boiling point difference gets remarkably large thereby between the α,α-difluoro ester of an objective product and the unsaturated ester of by-product, and a high purity product of the objective product is efficiently obtained by fractional distillation of a simple operation. The method is the practical method of producing the α,α-difluoro esters capable of solving a problem point in a prior technique. COPYRIGHT: (C)2012,JPOandINPIT
Synthesis of fluorinated and nonfluorinated tebufenpyrad analogues for the study of anti-angiogenesis MOA
Roman, Raquel,Navarro, Antonio,Wodka, Dariusz,Alvim-Gaston, Maria,Husain, Saba,Franklin, Natalie,Simon-Fuentes, Antonio,Fustero, Santos
, p. 1027 - 1036 (2014/10/15)
In this contribution we report the synthesis of fluorinated and nonfluorinated tebufenpyrad analogues to explore potential druglike properties through the phenotypic screening as part of the Lilly Open Innovation Drug Discovery (OIDD) program.
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)- 6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8-(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity
Dow, Robert L.,Carpino, Philip A.,Hadcock, John R.,Black, Shawn C.,Iredale, Philip A.,DaSilva-Jardine, Paul,Schneider, Steven R.,Paight, Ernest S.,Griffith, David A.,Scott, Dennis O.,O'Connor, Rebecca E.,Nduaka, Chudy I.
supporting information; experimental part, p. 2652 - 2655 (2010/03/03)
We report the design, synthesis, and structure-activity relationships of novel bicyclic lactam-based cannabinoid type 1 (CB1) receptor antagonists. Members of these series are potent, selective antagonists in in vitro/in vivo efficacy models of CB1 antagonism and exhibit robust oral activity in rodent models of food intake. These efforts led to the identification of 19d, which has been advanced to human clinical trials for weight management.
Improved regioselectivity in pyrazole formation through the use of fluorinated alcohols as solvents: Synthesis and biological activity of fluorinated tebufenpyrad analogs
Fustero, Santos,Roman, Raquel,Sanz-Cervera, Juan F.,Simon-Fuentes, Antonio,Cunat, Ana C.,Villanova, Salvador,Murguia, Marcelo
, p. 3523 - 3529 (2008/09/20)
(Chemical Equation Presented) The preparation of N-methylpyrazoles is usually accomplished through reaction of a suitable 1,3-diketone with methylhydrazine in ethanol as the solvent. This strategy, however, leads to the formation of regioisomeric mixtures of N-methylpyrazoles, which sometimes are difficult to separate. We have determined that the use of fluorinated alcohols such as 2,2,2-trifluoroethanol (TFE) and 1,1,1,3,3,3-hexafluoro-2-propanol (HFIP) as solvents dramatically increases the regioselectivity in the pyrazole formation, and we have used this modification in a straightforward synthesis of fluorinated analogs of Tebufenpyrad with acaricide activity.
Process for Preparing Bicyclic Pyrazolyl
-
Page/Page column 13, (2010/11/28)
A process for preparing compounds of Formula (I) is described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of disease linked to the mediation of the cannabinoid receptors in animals.
Bicyclic pyrazolyl and imidazolyl compounds and uses thereof
-
Page/Page column 31, (2010/02/11)
Compounds of Formula (I) are described herein. The compounds have been shown to act as cannabinoid receptor ligands and are therefore useful in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals.
MEDICINAL COMPOSITIONS
-
, (2008/06/13)
The present invention relates to an agent for the prophylaxis or treatment of pain, an agent for suppressing activation of osteoclast, and an inhibitor of osteoclast formation, which contains a p38 MAP kinase inhibitor and/or a TNF-α production inhibitor.
Substituted 1,3-thiazole compounds, their production and use
-
, (2008/06/13)
(1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.
