- MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF PROLIFERATION DISORDERS
-
The invention provides compounds of formula I or pharmaceutically acceptable salt, solvate or hydrate thereof (I) wherein ring A represents group A-I or A- II (A-I, A-II) A1, A2, A3, A4 represent independently C(R4aa) or N, wherein no more than one of A1, A2, A3, and A4 represents N; A5 represents C(R4b) or N; B1, B2, B3 and B4 represent independently C(R3) or N, wherein no more than two of B1, B2, B3 and B4 represent N; n is 1 or 2; and R1, R2, R3, R4a and R4aa and R4b are as defined in the claims, as well as methods of using the compounds to treat proliferation diseases, in particular cancer.
- -
-
Page/Page column 144
(2018/02/03)
-
- N-(1-Oxy-2-picolyl)oxalamic acids as a new type of O,O-ligands for the Cu-catalyzed N-arylation of azoles with aryl halides in water or organic solvent
-
N-(1-Oxy-pyridin-2-ylmethyl)oxalamic acids (L3-L5) were identified as novel efficient ligands for copper-catalyzed C-N cross-coupling of azoles and aryl halides in water. The N-arylation of imidazoles, indoles and pyrazoles proceeded with moderate to excellent yields and complete selectivity over aromatic amines and phenols. Moreover, L5, which is also efficient in organic solvent with low catalyst loading, can be used to promote the N-arylation reactions with water-sensitive materials. The catalytic mechanism was proposed based on the results of several verification experiments which indicated that the ligands as new-type chelators may coordinate to Cu(i) with two oxygen atoms of N-oxide and amide in the coupling process. This journal is
- Wang, Yongbin,Zhang, Yu,Yang, Beibei,Zhang, Ao,Yao, Qizheng
-
p. 4101 - 4114
(2015/03/30)
-
- Chiral amine-imine ligands based on trans-2,5-disubstituted pyrrolidines and their application in the palladium-catalyzed allylic alkylation
-
A series of amine-imine bidentate ligands based on a trans-2,5-disubstituted pyrrolidine and pyridine moieties have been prepared. The use of these ligands in the palladium-catalyzed allylic alkylation reaction of rac-(E)-1,3-diphenylprop-2-enyl acetate is reported. The results suggest that these ligands are good catalyst precursors for the reaction. Electronic modification on the pyridine ring of the ligands does not have a significant effect on the enantioselectivity of the reaction but does on the reaction rate, while structural modification on either the pyridine or the pyrrolidine moiety affords dramatic changes on the outcome of the stereochemistry. Evidence from various studies suggested that during the palladium-catalyzed allylic alkylation reaction, nucleophilic attack onto the 1,3-diphenylallyl moiety in the transition state occurs mainly trans to the pyridine ring of the less stable conformation of the palladium complexes.
- Chen, Hongfeng,Sweet, James A.,Lam, Kin-Chung,Rheingold, Arnold L.,McGrath, Dominic V.
-
experimental part
p. 1672 - 1682
(2009/12/04)
-
- Method for labelling phosphorylated peptides, complex compounds used in the methods, process for producing the same, and their intermediates
-
Provided are a method for easily detecting phosphorylated peptides, namely, proteins, in samples derived from living organisms or the like, a method for selectively adsorbing the phosphorylated peptides, and compounds that are highly coordinated to the phosphorylated peptides and usable in the methods. The complex compound is represented by the formula: wherein X is a linker moiety, and Y is a labeling group. The compound (I) is highly coordinated to a phosphorylated peptide. and has a labeling group. Accordingly, with use of the compound (I), the phosphorylated peptide can be easily identified.
- -
-
-