42518-98-9Relevant articles and documents
Syntheses of [14C]BAY 59-7939 and its radiolabeled metabolite M-4
Pleiss,Seidel,Grosser
, p. 929 - 934 (2006)
BAY 59-7939 is a novel, oral, direct Factor Xa inhibitor in clinical development for the prevention and treatment of thromboembolic diseases. Radiolabeled BAY 59-7939 was required for drug absorption, distribution, metabolism and excretion (ADME studies). The BAY 59-7939 was labeled with carbon-14 in the carboxamide group in one step in an overall radiochemical yield of 85% starting from 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl] phenyl}mor-pholin-3-one and 5-chlorothiophene-2-[14C]carboxylic acid. The radiolabeled metabolite M-4 was prepared in 77% yield starting from [1-14C]glycine and 5-chlorothiophene-5-carboxylic acid. Copyright
Benzo[1,2-b:4,5- b ′]diselenophene-fused nonfullerene acceptors with alternative aromatic ring-based and monochlorinated end groups: A new synergistic strategy to simultaneously achieve highly efficient organic solar cells with the energy loss of 0.49 eV
Wan, Shi-Sheng,Xu, Xiaopeng,Wang, Jin-Liang,Yuan, Gui-Zhou,Jiang, Zhao,Ge, Gao-Yang,Bai, Hai-Rui,Li, Zheng,Peng, Qiang
, p. 11802 - 11813 (2019)
Herein, a new synergistic strategy using electron-rich core units and alternative aromatic structure-based 1,1-dicyanomethylene-3-indanone (IC) end-groups for nonfullerene PSCs was reported and investigated in an attempt to simultaneously obtain excellent PCE with extremely low Eloss. Specifically, two benzo[1,2-b:4,5-b′]diselenophene-based, A-D-A-type chlorinated NF-SMAs (BDSeThCl and BDSePhCl) were synthesized, which were linked with a new 2-chlorothienyl-based IC and a conventional monochlorinated phenyl-based IC as end-groups, respectively. BDSePhCl exhibited a wider and red-shifted absorption and downshifted energy levels than BDSeThCl. The blend films of BDSePhCl:PM7 exhibited better charge generation properties, more suitable phase separation, and more balanced charge mobilities as compared to those of BDSeThCl:PM7. Therefore, compared to the BDSeThCl:PM7 blends with the best PCE of 11.91% and the Eloss of 0.58 eV, the optimal BDSePhCl:PM7 blends showed the enhanced PCE of 13.68% with the reduced Eloss of 0.49 eV. Notably, the excellent PCE of 13.68% is the highest value recorded to date for A-D-A-type NF-SMAs with a monochlorinated IC group in binary PSCs. The Eloss of 0.49 eV is the lowest value reported to date for A-D-A-type NF-SMAs in binary PSCs with the PCE > 13%. These results demonstrate that tailoring of the monochlorinated aromatic ring-based IC is an effective strategy to simultaneously improve the PCE and reduce the Eloss in binary PSCs.
Nickel-Catalyzed Oxidative Transamidation of Tertiary Aromatic Amines with N -Acylsaccharins
Liu, Shengzhang,Yang, Lingyun,Tao, Jiasi,Yu, Weijie,Wang, Tao,Fu, Junkai
supporting information, p. 1642 - 1646 (2021/06/21)
The use of tertiary amines as surrogates for secondary amines has prominent advantages in terms of stabilization and ease of handling. A Ni-catalyzed transamidation of N -acylsaccharins with tertiary aromatic amines is reported. By using tert -butyl hydroperoxide as the terminal oxidant, this reaction permits selective cleavage of the C(sp 3)-N bonds of unsymmetrical tertiary aromatic amines depending on the sizes of the alkyl substituents.
Highly regioselective and stereoselective synthesis of C-Aryl glycosidesvianickel-catalyzedortho-C-H glycosylation of 8-aminoquinoline benzamides
Chen, Xi,Ding, Ya-Nan,Gou, Xue-Ya,Liang, Yong-Min,Luan, Yu-Yong,Niu, Zhi-Jie,Shi, Wei-Yu,Zhang, Zhe,Zheng, Nian
supporting information, p. 8945 - 8948 (2021/09/10)
C-Aryl glycosides are of high value as drug candidates. Here a novel and cost-effective nickel catalyzedortho-CAr-H glycosylation reaction with high regioselectivity and excellent α-selectivity is described. This method shows great functional group compatibility with various glycosides, showing its synthetic potential. Mechanistic studies indicate that C-H activation could be the rate-determining step.
