40771-41-3Relevant academic research and scientific papers
Grignard-Reagent-Promoted Desulfonylation/Intramolecular Coupling for the Synthesis of 2-(1-Fluorovinyl)pyridines
Jiang, Gaoxi,Kang, Lei,Qian, Jinlong,Yang, Huameng,Zhang, Jinlong
supporting information, p. 9118 - 9122 (2020/12/02)
A novel process involving Grignard-reagent-promoted desulfonylation/intramolecular coupling of readily available α-fluoro-α,β-unsaturated-(2-pyridyl)sulfones was realized that provided a series of polysubstituted 2-(1-fluorovinyl)pyridines in good yields. The intrinsic coordination between pyridine and Mg(II) along with the "negative fluorine effect"of the substrates should play the key role for the smooth transformation in the absence of transition-metal catalysts.
Addition of novel benzylmagnesium “ate” complexes of BnR2MgLi type to 2-(thio)pyridones and related compounds
So?nicki, Jacek G.,Idzik, Tomasz,Borzyszkowska, Aleksandra,Wróblewski, Emil,Maciejewska, Gabriela,Struk, ?ukasz
supporting information, p. 481 - 493 (2017/01/13)
Novel benzylation reagents BnR2MgLi were obtained by mixing benzylmagnesium chloride (BnMgCl) and appropriate organolithium compounds (RLi). As BnR2MgLi complexes are more nucleophilic than the parent Grignard compound they enabled regioselective C6-addition to electrophilic N-substituted 2-(thio)-pyridones and C4-addition to poorly reactive NH 2-(thio)pyridones in high and good yields, respectively. Thus, the application of these new reagents in efficient synthesis of 6-benzyl-3,6-dihydro- and 4-benzyl-3,4-dihydropyridin-2(1H)-ones is described. The prospect of wider application of BnR2MgLi in 1,4-addition to other electrophiles, comprising six-membered α,β-unsaturated systems is also presented.
Silver-induced self-immolative Cl-F exchange fluorination of arylsulfur chlorotetrafluorides: Synthesis of arylsulfur pentafluorides
Cui, Benqiang,Jia, Shichong,Tokunaga, Etsuko,Saito, Norimichi,Shibata, Norio
supporting information, p. 12738 - 12741 (2017/12/06)
A novel strategy for the synthesis of arylsulfur pentafluorides by silver carbonate-induced Cl-F exchange fluorination of arylsulfur chlorotetrafluorides is reported. This fluorination does not require any exogenous fluoride sources. Rather, the reaction proceeds via the self-immolation of the substrate Ar-SF4Cl.
IF5 affects the final stage of the Cl-F exchange fluorination in the synthesis of pentafluoro-λ6-sulfanyl-pyridines, pyrimidines and benzenes with electron-withdrawing substituents
Cui, Benqiang,Kosobokov, Mikhail,Matsuzaki, Kohei,Tokunaga, Etsuko,Shibata, Norio
supporting information, p. 5997 - 6000 (2017/07/10)
A difficult chlorine-fluorine (Cl-F) exchange fluorination reaction in the final stage of the preparation of pentafluoro-λ6-sulfanyl-(hetero)arenes having electron-withdrawing substituents has now been elucidated through the use of iodine pentafluoride. A major side-reaction of C-S bond cleavage was sufficiently inhibited by the potential interaction between F and I with a halogen bonding.
Discovery of MK-3168: A PET tracer for imaging brain fatty acid amide hydrolase
Liu, Ping,Hamill, Terence G.,Chioda, Marc,Chobanian, Harry,Fung, Selena,Guo, Yan,Chang, Linda,Bakshi, Raman,Hong, Qingmei,Dellureficio, James,Lin, Linus S.,Abbadie, Catherine,Alexander, Jessica,Jin, Hong,Mandala, Suzanne,Shiao, Lin-Lin,Li, Wenping,Sanabria, Sandra,Williams, David,Zeng, Zhizhen,Hajdu, Richard,Jochnowitz, Nina,Rosenbach, Mark,Karanam, Bindhu,Madeira, Maria,Salituro, Gino,Powell, Joyce,Xu, Ling,Terebetski, Jenna L.,Leone, Joseph F.,Miller, Patricia,Cook, Jacquelynn,Holahan, Marie,Joshi, Aniket,O'Malley, Stacey,Purcell, Mona,Posavecz, Diane,Chen, Tsing-Bau,Riffel, Kerry,Williams, Mangay,Hargreaves, Richard,Sullivan, Kathleen A.,Nargund, Ravi P.,DeVita, Robert J.
supporting information, p. 509 - 513 (2013/07/26)
We report herein the discovery of a fatty acid amide hydrolase (FAAH) positron emission tomography (PET) tracer. Starting from a pyrazole lead, medicinal chemistry efforts directed toward reducing lipophilicity led to the synthesis of a series of imidazole analogues. Compound 6 was chosen for further profiling due to its appropriate physical chemical properties and excellent FAAH inhibition potency across species. [11C]-6 (MK-3168) exhibited good brain uptake and FAAH-specific signal in rhesus monkeys and is a suitable PET tracer for imaging FAAH in the brain.
NOVEL PHENYLPYRROLE DERIVATIVE
-
Page/Page column 157, (2010/11/03)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group α, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group α or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group α, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group α consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydroxy group(s), a C1-C6 alkylsulfonyl group, and a group represented by the formula -V-NR5R6 (wherein, V represents a carbonyl group or a sulfonyl group, and R5 and R6 may be the same or different and respectively represent a hydrogen atom or a C1-C6 alkyl group, or R5 and R6 together with the nitrogen atom bonded thereto form a 4- to 6-membered saturated heterocycle that may be substituted with 1 or 2 group(s) independently selected from a C1-C6 alkyl group and a hydroxy group, and the 4- to 6-membered saturated heterocycle may further contain one oxygen atom or nitrogen atom)].
IMIDAZOLE DERIVATIVES USEFUL AS MODULATORS OF FAAH AND AS FAAH IMAGING AGENTS
-
Page/Page column 30, (2010/09/18)
The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds
IMIDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
-
Page/Page column 29, (2010/01/07)
The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
HETEROCYCLIC METHYL SULFONE DERIVATIVE
-
Page/Page column 23, (2010/11/08)
Provided is a compound capable of inhibiting production or secretion of β amyloid protein. A compound represented by the following formula (1): (wherein, R1 represents a heterocyclic group which may have a substituent, R2 represents a cyclic hydrocarbon group which may have a substituent or a heterocyclic group which may have a substituent, R3 represents a cyclic hydrocarbon group which may have a substituent or a heterocyclic group which may have a substituent, R4 represents a hydrogen atom or a C1-6 alkyl group, and X represents -S-,-SO- or -SO2-) an N-oxide or S-oxide thereof; a salt thereof; or a solvate thereof; and a medicament containing any of them.
BETA-AMYLOID PROTEIN PRODUCTION/SECRETION INHIBITORS
-
Page 129, (2010/02/08)
Provided are novel compounds having an inhibitory activity against production or secretion of β-amyloid protein. They embrace compounds represented by the following formula (1): and capable of being replaced with a variety of substituents; and salts thereof, and solvates of any one of them.
