- Pd-PEPPSI-IPentAn Promoted Deactivated Amination of Aryl Chlorides with Amines under Aerobic Conditions
-
We report herein a highly efficient Pd-catalyzed amination by "bulky-yet-flexible" Pd-PEPPSI-IPentAn complexes. The relationship between the N-heterocyclic carbenes (NHCs) structure and catalytic properties was discussed. Sterically hindered (hetero)aryl chlorides and a variety of aliphatic and aromatic amines can be applied in this cross-coupling, which smoothly proceeded to provide desired products. The operationally simple protocol highlights the rapid access to CAr-N bond formation under mild conditions without the exclusion of air and moisture.
- Huang, Fei-Dong,Xu, Chang,Lu, Dong-Dong,Shen, Dong-Sheng,Li, Tian,Liu, Feng-Shou
-
p. 9144 - 9155
(2018/07/21)
-
- Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use
-
Compounds that interact with the histamine H4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H4 receptor, e.g. inflammation, are of formula (I) wherein Q is CR1 or N; X is CR2 or N, provided that Q and X are not both N; Y is CR3 or N; Z is CH or N; R1, R2, R3, R4, R5 and R6 are independently H, F, Cl, Br, I, or a hydrocarbon group which optionally contains one or more heteroatoms; and R7 is a heterocyclic radical including one or more N atoms; or a pharmaceutically acceptable salt, ester or solvate thereof.
- -
-
Page/Page column 11
(2010/02/17)
-
- Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo
-
Using a previously reported flexible alignment model we have designed, synthesized, and evaluated a series of compounds at the human histamine H 4 receptor (H4R) from which 2-(4-methyl-piperazin-l-yl)- quinoxaline (3) was identified as a new lead structure for H4R ligands. Exploration of the structure-activity relationship (SAR) of this scaffold led to the identification of 6,7-dichloro 3-(4-methylpiperazin-l-yl) quinoxalin-2(1H)-one (VUF 10214, 57) and 2-benzyl-3-(4-methyl-piperazin-l-yl) quinoxaline (VUF 10148, 20) as potent H4R ligands with nanomolar affinities. In vivo studies in the rat reveal that compound 57 has significant anti-inflammatory properties in the carrageenan-induced paw-edema model.
- Smits, Rogier A.,Lim, Herman D.,Hanzer, Agnes,Zuiderveld, Obbe P.,Guaita, Elena,Adami, Maristella,Coruzzi, Gabriella,Leurs, Rob,De Esch, Iwan J. P.
-
p. 2457 - 2467
(2008/12/22)
-
- Phosphorus Pentoxide in Organic Synthesis XXXII A New Synthesis of Quipazine and Its N-Methyl Derivatives
-
2-(4-Methyl-1-piperazinyl)quinolines 1 were prepared by heating acetanilides and N,N-dialkylformamides with a mixture of P2O5 and N-methylpiperazine at 250 deg C.Quipazine was obtained by von Braun degradation of 1a to N-cyano-N'-(2-quinolyl)piperazine (2) and hydrolysis in sulfuric acid.
- Jensen, Jorgen A.,Pedersen, Erik B.
-
p. 1088 - 1092
(2007/10/02)
-