92039-31-1Relevant articles and documents
Cu-Catalyzed alkylation-cyanation type difunctionalization of styrenes with aliphatic aldehydes and TMSCN via decarbonylation
Zhou, Yu-Ling,Chen, Jun-Jia,Cheng, Jing,Yang, Luo
supporting information, p. 1231 - 1235 (2022/02/19)
A copper-catalyzed decarbonylative alkylation-cyanation of styrene derivatives with aliphatic aldehydes and trimethylsilyl cyanide to provide chain elongated nitriles is reported. Using TBHP as an oxidant and free radical initiator, the reaction can smoothly convert abundant α-di-substituted, α-mono-substituted and linear aliphatic aldehydes into the corresponding 3°, 2° and 1° alkyl radicals to initiate the subsequent radical-type difunctionalization of various styrenes.
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.