159800-47-2Relevant academic research and scientific papers
Direct α-Tertiary Alkylations of Ketones in a Combined Copper–Organocatalyst System
Kurose, Ayako,Ishida, Yuto,Hirata, Goki,Nishikata, Takashi
supporting information, p. 10620 - 10625 (2021/04/09)
Herein, we report an efficient method for the tertiary alkylation of a ketone by using an α-bromocarbonyl compound as the tertiary alkyl source in a combined Cu-organocatalyst system. This dual catalyst system enables the addition of a tertiary alkyl radical to an enamine. Mechanistic studies revealed that the catalytically generated enamine is a key intermediate in the catalytic cycle. The developed method can be used to synthesize substituted 1,4-dicarbonyl compounds containing quaternary carbons bearing various alkyl chains.
Copper-Catalyzed Alkylation of Silyl Enol Ethers with Sterically Hindered α-Bromocarbonyls: Access to the Histamine H3Receptor Antagonist
Li, Dengke
, p. 609 - 618 (2020/12/23)
A general and efficient copper-catalyzed alkylation of silyl enol ethers with functionalized alkyl bromides has been developed for the synthesis of the sterically hindered γ-ketoesters. The transformation was induced through C(sp3)-halogen activation of commercially available sterically hindered alkyl bromides under mild conditions in good results. The strategy could be used for the synthesis of biologically active histamine H3 receptor (H3R) antagonist for medicinal purposes.
Conversion of γ-bicyclic lactams to 4,5-dihydro-2H-pyridazin-3-ones
Lim, Yu Jin,Angela, Mia,Buonora, Paul T.
, p. 7799 - 7801 (2007/10/03)
Bicyclic lactams are uniquely suited as precursors for the synthesis of chiral substituted 4,5-dihydro-2H-pyridazinones. This paper describes the development of a method for the direct conversion of unsubstituted and 4-substituted γ-bicyclic lactams to 4,5-dihydro-2H-pyridazin-3-ones and 2-phenyl-4,5-dihydro-2H-pyridazin-3-ones.
Nonsteroidal Progesterone Receptor Ligands. 2. High-Affinity Ligands with Selectivity for Bone Cell Progesterone Receptors
Combs, Donald W.,Reese, Kimberly,Cornelius, Lyndon A. M.,Gunnet, Joseph W.,Cryan, Ellen V.,et al.
, p. 4880 - 4884 (2007/10/03)
A novel series of nonsteroidal heterocycles was discovered which display cell-type selective, high-affinity (nanomolar) binding to the progesterone receptors from TE85 osteosarcoma cells but > 1 μM binding affinity to the progesterone receptors from T47D and ZR75 human breast carcinpma cells.Structure-activity relationships were developed for a set of these compounds, and a representative analog 1-(3,4-dichlorobenzoyl)-3-phenyl-1,4,5,6-tetrahydropyridazine (1i, RWJ 25333) was chosen for further evaluation.RWJ 25333 stimulated the in vitro proliferation of human osteoblast-like cells but not human breast cells.
