- Nickel-catalyzed Negishi cross-coupling reactions of secondary alkylzinc halides and aryl iodides
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A general Ni-catalyzed process for the cross-coupling of secondary alkylzinc halides and aryl/heteroaryl iodides has been developed. This is the first process to overcome the isomerization and β-hydride elimination problems that are associated with the use of secondary nucleophiles, and that have limited the analogous Pd-catalyzed systems. The impact of salt additives was also investigated. It was found that the presence of LiBF4 dramatically improves both isomeric retention and yield for challenging substrates.(Figure Presented)
- Joshi-Pangu, Amruta,Ganesh, Madhu,Biscoe, Mark R.
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supporting information; experimental part
p. 1218 - 1221
(2011/04/27)
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- Synthesis and evaluation of 4-alkylanilines as mammary tumor inhibiting aromatase inhibitors
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The 4-alkylanilines 1-20 were synthesized to elucidate the importance of the glutarimide moiety for the aromatase inhibiting activity of aminoglutethimide [3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione, AG], the only non-steroidal aromatase inhibitor which is commercially available at present. The most interesting compounds were the (4-aminophenyl)cycloalkanes 4-6 (4, c-pentyl; 5, c-hexyl; 6, c-heptyl) and the 1-alkyl-1-(4-aminophenyl)cyclohexanes 1-3 (1, CH3; 2, C2H5; 3, n-C3H7). Derivatives 1-6 are stronger inhibitors of human placental aromatase than AG exhibiting relative potencies from 1.5 to 2.7 (AG≡1). For selectivity of action, the inhibition of desmolase (cholesterol side chain cleavage enzyme) was determined. Compounds 1-3 showed an inhibition comparable to AG, whereas compounds 4-6 exhibited no effect on desmolase. Being more potent and selective aromatase inhibitors in vitro, compounds 4-6, however, were not superior to AG in vivo, when the reduction of plasma estradiol concentration and the tumor inhibiting activity (PMSG-primed SD rats and DMBA-induced mammary carcinoma of the SD rat, postmenopausal model) were concerned.
- Hartmann,Batzl
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p. 537 - 544
(2007/10/02)
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- 9-(P-phenylazoanilino)-7-methyl-1H-imidazo[4,5-f]quinolines
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A series of 9-(substituted amino)imidazo[4,5-f]quinolines are effective anthelmintic agents; particularly in respect to the tapeworm Hymenolepis nana.
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