28781-85-3Relevant articles and documents
METHOD FOR PREPARING FLUOROORGANIC COMPOUNDS
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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
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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
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.
