36716-70-8Relevant academic research and scientific papers
Shuttle arylation by Rh(I) catalyzed reversible carbon–carbon bond activation of unstrained alcohols
Lutz, Marius D.R.,Gasser, Valentina C.M.,Morandi, Bill
, p. 1108 - 1119 (2021/04/19)
The advent of transfer hydrogenation and borrowing hydrogen reactions paved the way to manipulate simple alcohols in previously unthinkable manners and circumvented the need for hydrogen gas. Analogously, transfer hydrocarbylation could greatly increase the versatility of tertiary alcohols. However, this reaction remains unexplored because of the challenges associated with the catalytic cleavage of unactivated C–C bonds. Herein, we report a rhodium(I)-catalyzed shuttle arylation cleaving the C(sp2)–C(sp3) bond in unstrained triaryl alcohols via a redox-neutral β-carbon elimination mechanism. A selective transfer hydrocarbylation of substituted (hetero)aryl groups from tertiary alcohols to ketones was realized, employing benign alcohols as latent C-nucleophiles. All preliminary mechanistic experiments support a reversible β-carbon elimination/migratory insertion mechanism. In a broader context, this novel reactivity offers a new platform for the manipulation of tertiary alcohols in catalysis.
4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2
-
Page/Page column 82, (2010/11/03)
The present invention comprises compounds of Formula (I): wherein: X, R1, R2, R3, and R4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2
Xue, Chu-Biao,Wang, Anlai,Meloni, David,Zhang, Ke,Kong, Ling,Feng, Hao,Glenn, Joseph,Huang, Taisheng,Zhang, Yingxin,Cao, Ganfeng,Anand, Rajan,Zheng, Changsheng,Xia, Michael,Han, Qi,Robinson,Storace, Lou,Shao, Lixin,Li, Mei,Brodmerkel, Carrie M.,Covington, Maryanne,Scherle, Peggy,Diamond, Sharon,Yeleswaram, Swamy,Vaddi, Kris,Newton, Robert,Hollis, Greg,Friedman, Steven,Metcalf, Brian
scheme or table, p. 7473 - 7478 (2011/01/12)
Rational design based on a pharmacophore of CCR2 antagonists reported in the literature identified lead compound 9a with potent inhibitory activity against human CCR2 (hCCR2) but moderate activity against murine CCR2 (mCCR2). Modification on 9a led to the
4'-Fluoro-4-{[4-(phenyl)cyclohexyl]amino}butyrophenones and the salts thereof
-
, (2008/06/13)
This invention relates to novel 4-phenylcyclohexylamines embraced by the formula SPC1 Wherein ? is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof; R is selected from the group consisting of alkyl of from one through four carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, nitro and alkoxy of from one through four carbon atoms; R' and R1 are selected from the group consisting of hydrogen and alkyl of from one through four carbon atoms; R2 is selected from the group consisting of hydrogen, alkyl of from one through four carbon atoms, alkanoyl of from one through three carbon atoms, alkylsulfonyl of from one through three carbon atoms, arylsulfonyl of from six through ten carbon atoms, alkylcarbamoyl wherein alkyl is from one through four carbon atoms, alkoxycarbonyl wherein alkyl is from one through four carbon atoms, ring monosubstituted aroylalkyl wherein the substituents have the same meaning as R, above, aryl is from six through ten carbon atoms and alkyl is from one through six carbon atoms and bis (ring monosubstituted) arylalkyl wherein the substituents have the same meaning as R, above, aryl is from six through ten carbon atoms and alkyl is from one through six carbon atoms; R1 and R2 when taken together with --N is a saturated heterocyclic amino radical selected from the group consisting of unsubstituted and monosubstituted pyrrolidino, piperidino, hexamethylenimino, morpholino and piperazino; and an acid addition salt thereof. It also relates to intermediates and processes for the preparation of the aforesaid novel compounds (1) and novel derivatives thereof. The systemic administration to humans and animals of the novel compounds (1) depresses their central nervous systems.
4'-Fluoro-4-{[4-(phenyl)-4-alkoxy-cyclo-hexyl]amino}butyrophenones and the salts thereof
-
, (2008/06/13)
This invention relates to novel 4-(substituted alkoxy)-4-(substituted phenyl)cyclohexylamines embraced by the formula SPC1 Wherein ? is a generic expression denoting cis and trans stereoconfiguration and mixtures thereof, with the proviso that when the st
