364-11-4Relevant academic research and scientific papers
PROCESS FOR THE PREPARATION OF SUBSTITUTED BENZOTRIHALIDE
-
Page/Page column 8, (2016/06/06)
The present invention provides a process for the preparation of compound of Formula I; wherein X is selected from the group consisting of fluorine, chlorine, bromine and iodine; Y is selected from X and -NR1R2; R1 and R1, independent of each other, are selected from the group consisting of hydrogen, C1-4 alkyl and –COR; R is C1-4 alkyl.
Silver-Catalyzed C-H Trifluoromethylation of Arenes Using Trifluoroacetic Acid as the Trifluoromethylating Reagent
Shi, Guangfa,Shao, Changdong,Pan, Shulei,Yu, Jingxun,Zhang, Yanghui
supporting information, p. 38 - 41 (2015/07/28)
Direct trifluoromethylation of arenes using TFA as the trifluoromethylating reagent was achieved with Ag as the catalyst. This reaction not only provides a new protocol for aryl C-H trifluoromethylation, but the generation of CF3· from TFA may prove useful in other contexts and could potentially be extended to other trifluoromethylation reactions. (Chemical Equation Presented).
Identification and development of biphenyl substituted iminosugars as improved dual glucosylceramide synthase/neutral glucosylceramidase inhibitors
Ghisaidoobe, Amar T.,Van Den Berg, Richard J. B. H. N.,Butt, Saleem S.,Strijland, Anneke,Donker-Koopman, Wilma E.,Scheij, Saskia,Van Den Nieuwendijk, Adrianus M. C. H.,Koomen, Gerrit-Jan,Van Loevezijn, Arnold,Leemhuis, Mark,Wennekes, Tom,Van Der Stelt, Mario,Van Der Marel, Gijsbert A.,Van Boeckel, Constant A. A.,Aerts, Johannes M. F. G.,Overkleeft, Herman S.
supporting information, p. 9096 - 9104 (2015/03/14)
This work details the evaluation of a number of N-alkylated deoxynojirimycin derivatives on their merits as dual glucosylceramide synthase/neutral glucosylceramidase inhibitors. Building on our previous work, we synthesized a series of d-gluco and l-ido-configured iminosugars N-modified with a variety of hydrophobic functional groups. We found that iminosugars featuring N-pentyloxymethylaryl substituents are considerably more potent inhibitors of glucosylceramide synthase than their aliphatic counterparts. In a next optimization round, we explored a series of biphenyl-substituted iminosugars of both configurations (d-gluco and l-ido) with the aim to introduce structural features known to confer metabolic stability to drug-like molecules. From these series, two sets of molecules emerge as lead series for further profiling. Biphenyl-substituted l-ido-configured deoxynojirimycin derivatives are selective for glucosylceramidase and the nonlysosomal glucosylceramidase, and we consider these as leads for the treatment of neuropathological lysosomal storage disorders. Their d-gluco-counterparts are also potent inhibitors of intestinal glycosidases, and because of this characteristic, we regard these as the prime candidates for type 2 diabetes therapeutics.
ALPHA-CARBOLINES FOR THE TREATMENT OF CANCER
-
Page/Page column 90, (2013/12/03)
The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in
Analogues of orphan nuclear receptor small heterodimer partner ligand and apoptosis inducer (E)-4-[3-(1-adamantyl)-4-hydroxyphenyl]-3-chlorocinnamic acid. 2. Impact of 3-chloro group replacement on inhibition of proliferation and induction of apoptosis of
Xia, Zebin,Correa, Ricardo G.,Das, Jayanta K.,Farhana, Lulu,Castro, David J.,Yu, Jinghua,Oshima, Robert G.,Fontana, Joseph A.,Reed, John C.,Dawson, Marcia I.
experimental part, p. 233 - 249 (2012/03/10)
The parent phenol of adapalene and its (E)-cinnamic acid analogue were found to induce cancer cell apoptosis but cause adverse systemic effects when administered to mice. In contrast, their respective 5-Cl- and 3-Cl-substituted analogues had their adverse
Expedient synthesis of N-fused indoles: A C-F activation and C-H insertion approach
Fuchibe, Kohei,Kaneko, Tsukasa,Mori, Keiji,Akiyama, Takahiko
supporting information; experimental part, p. 8070 - 8073 (2010/02/27)
Easy does it: A wide range of N-fused indole skeletons, which are core structures of many biologically potent molecules, are successfully furnished by a niobiumcatalyzed C(sp3)-H insertion reaction (see picture). The precursors are readily prepared by a palladium-catalyzed amination reaction of bromotrifluorotoluenes with cyclic amines.
Insecticidal benzofuran derivatives
-
, (2008/06/13)
A compound of the formula STR1 wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl, alkenyl and alkynyl of up to 8 carbon atoms, optionally substituted cycloalkyl or cycloalkenyl of up to 8 carbon atoms, optionally substituted aryl of 6 to 18 carbon atoms, optionally substituted aralkyl of 7 to 24 carbon atoms, optionally substituted benzoyl and optionally substituted heterocycle, the optional substituents being at least one member of the group consisting of halogen, phenoxy, thiazolyl, alkyl and alkoxy of 1 to 6 carbon atoms and haloalkyl, Alk1 and Alk2 are individually optionally substituted alkyl of 1 to 8 carbon atoms, X is --O-- or --S-- and R' is hydrogen or halogen in any position on the phenyl and the geometry of the double bond is E or Z or a mixture of E and Z and having useful pesticidal properties.
