14149-34-9Relevant academic research and scientific papers
Copper-Catalyzed Enantioselective Cyano(Fluoro)Alkylation of Alkenes
Bao, Hongli,Israr, Muhammad,Li, Yajun,Xiong, Haigen
, (2020)
A copper-catalyzed asymmetric cyano(fluoro)alkylation reaction of alkenes is reported. A range of chiral fluoroalkyl cyanides were obtained in high yields and excellent enantiomeric excess from readily available chemicals. The method uses fluoroalkyl iodi
C3-CARBON LINKED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN DEGRADATION
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Page/Page column 350; 351, (2017/12/05)
This invention provides Degronimers that have carbon-linked E3 Ubiquitin Ligase targeting moieties (Degrons), which can be linked to a targeting ligand for a protein that has been selected for in vivo degradation, and methods of use and compositions thereof as well as methods for their preparation.
Synthesis of heterocyclic compounds using amidines as their ene-1,1-diamine tautomers. I. Synthesis of 4,5-dihydro-3H-pyridin-2-one, 3,4-dihydropyrrol-2- one and 1,3-dihydropyrrol-2-one derivatives by the reaction of amidines with α,β-unsaturated esters
Ito, Kunio,Kizuka, Yoshiko,Hirano, Yuji
, p. 583 - 588 (2007/10/03)
N-t-Butylacetamidines 1 on heating with methyl acrylate (2) at 200° gave the 4,5-dihydro-3H-pyridin-2-one derivatives 5. Michael addition of the acetamidines 1 as their ene-1,1-diamine tautomers 1′ to 2 and the subsequent cyclization of the adducts gave derivatives 5. Amidines 1 on reaction with trimethyl ethylenetricarboxylate (9) or dimethyl acetylenedicarboxylate (12) afforded 3,4-dihydropyrrol-2-one 11 or 1,3-dihydropyrrol-2-one derivatives 13.
Aromatase Inhibitors. Synthesis and Evaluation of Mammary Tumor Inhibiting Activity of 3-Alkylated 3-(4-Aminophenyl)piperidine-2,6-diones
Hartmann, Rolf W.,Batzl, Christine
, p. 1362 - 1369 (2007/10/02)
The synthesis and biological evaluation of 3-alkyl-substituted 3-(4-aminophenyl)piperidine-2,6-diones as inhibitors of estrogen biosynthesis are described .In vitro compounds 4-14 showed a stronger inhibition of human placental aromatase compared to aminoglutethimide (AG, compound 3), which recently has become used for the treatment of hormone-dependent breast cancer.The most active derivative, compound 10, showed a 93-fold stronger inhibition than AG.With the exception of 5, 7, and 8, all other compounds exhibited similar or decreased inhibition of bovine adrenal desmolase compared to AG.Compounds 4 and 6-12 showed a stronger inhibition of the plasma estradiol concentration of pregnant mare serum gonadotropin (PMSG) primed Sprague-Dawley (SD) rats compared to the parent compound.Compounds 4, 6-8, 10, and 12 inhibited the testosterone-stimulated tumor growth of ovariectomized 9,10-dimethyl-1,2-benzanthracene (DMBA) tumor-bearing SD rats more strongly than AG.Being stronger and more selective inhibitors of the estrogen biosynthesis than AG, some of the newly developed derivatives of AG might be better candidates for the treatment of the hormone-dependent human breast cancer.
