- Α, α-difluoropropionic production of esters
-
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
- -
-
Paragraph 0154-0158
(2016/10/10)
-
- NOVEL INHIBITORS
-
The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N- terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
- -
-
Page/Page column 69; 125
(2014/09/29)
-
- Practical selective hydrogenation of α-fluorinated esters with bifunctional pincer-type ruthenium(II) catalysts leading to fluorinated alcohols or fluoral hemiacetals
-
Selective hydrogenation of fluorinated esters with pincer-type bifunctional catalysts RuHCl(CO)(dpa) 1a, trans-RuH2(CO)(dpa) 1b, and trans-RuCl2(CO)(dpa) 1c under mild conditions proceeds rapidly to give the corresponding fluorinated alcohols or hemiacetals in good to excellent yields. Under the optimized conditions, the hydrogenation of chiral (R)-2-fluoropropionate proceeds smoothly to give the corresponding chiral alcohol without any serious decrease of the ee value.
- Otsuka, Takashi,Ishii, Akihiro,Dub, Pavel A.,Ikariya, Takao
-
supporting information
p. 9600 - 9603
(2013/07/26)
-
- METHOD FOR PRODUCING -FLUOROALCOHOL
-
A production method of a β-fluoroalcohol includes performing a reaction of an α-fluoroester with hydrogen gas (H2) in the presence of a specific ruthenium complex (i.e. a ruthenium complex of the general formula [2], preferably a ruthenium complex of the general formula [4]). This production method can employ a suitable hydrogen pressure of 1 MPa or less by the use of such a specific ruthenium complex and does not require a high-pressure gas production facility when put in industrial practice. In addition, this production method can remarkably reduce the amount of catalyst used therein (to e.g. a substrate/catalyst ratio of 20,000) in comparison to the substrate/catalyst ratio conventional reduction of α-fluoroalcohol. It is possible by these reduction in hydrogen pressure and catalyst amount to largely reduce the production cost of the β-fluoroalcohol.
- -
-
Paragraph 0050
(2013/11/05)
-
- New bicyclic cannabinoid receptor-1 (CB1-R) antagonists
-
A series of conformationally constrained bicyclic derivatives derived from SR141716 was prepared and evaluated as hCB1-R antagonists and inverse agonists. Optimization of the structure-activity relationships around the 2,6-dihydro-pyrazolo[4,3-
- Carpino, Philip A.,Griffith, David A.,Sakya, Subas,Dow, Robert L.,Black, Shawn C.,Hadcock, John R.,Iredale, Philip A.,Scott, Dennis O.,Fichtner, Michael W.,Rose, Colin R.,Day, Robert,Dibrino, Joseph,Butler, Mary,DeBartolo, Demetria B.,Dutcher, Darrin,Gautreau, Denise,Lizano, Jeff S.,O'Connor, Rebecca E.,Sands, Michelle A.,Kelly-Sullivan, Dawn,Ward, Karen M.
-
p. 731 - 736
(2007/10/03)
-
- CANNABINOID RECEPTOR LIGANDS AND USES THEREOF
-
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
- -
-
-
- Cannabinoid receptor ligands and uses thereof
-
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
- -
-
-
- REACTION OF HYDROXY AND CARBONYL COMPOUNDS WITH SULFUR TETRAFLUORIDE. XIII. REACTIONS OF ALIPHATIC HYDROXY KETONES WITH SULFUR TETRAFLUORIDE
-
Aliphatic α-hydroxy ketones react with sulfur tetrafluoride to form trifluoroalkanes and difluoroalkyl fluorosulfinates.The action of sulfur tetrafluoride on 4-hydroxy-2-pentanone gives 2,2,4-trifluoropentane and 3-penten-2-one.
- Stepanov, I. V.,Burmakov, A. I.
-
-