101259-87-4Relevant articles and documents
Cyclometalated palladium pre-catalyst for N-alkylation of amines using alcohols and regioselective alkylation of sulfanilamide using aryl alcohols
Mamidala, Ramesh,Mukundam, Vanga,Dhanunjayarao, Kunchala,Venkatasubbaiah, Krishnan
supporting information, p. 2225 - 2233 (2017/03/24)
Simple pyrazole based palladacycle-phosphine with a high turnover has been developed and applied for the N-alkylation of amines and sulfanilamide using alcohols as substrates by hydrogen borrowing strategy. N-alkylation of primary and secondary amines resulted in high isolated yields at 100–130 °C, under solvent free conditions. More challenging secondary aliphatic as well as aromatic alcohols were also successfully utilized as alkylating agents under similar reaction conditions. The turn over number reached up to 43000 for N-benzylation of aniline using benzyl alcohol. Notably, regioselective N-alkylation of 2-aminobenzothiazole and 4-aminobenzenesulfonamide to the corresponding 2-N-(alkylamino)azoles and 4-amino-(N-alkyl)benzenesulfonamides using alcohols as alkylating agents have been achieved using our new pre-catalyst-phosphine system.
Design, synthesis, and biological activity of novel PPARγ ligands based on rosiglitazone and 15d-PGJ2
Usui, Shinya,Suzuki, Takayoshi,Hattori, Yoshifumi,Etoh, Kazuma,Fujieda, Hiroki,Nishizuka, Makoto,Imagawa, Masayoshi,Nakagawa, Hidehiko,Kohda, Kohfuku,Miyata, Naoki
, p. 1547 - 1551 (2007/10/03)
To develop novel PPARγ ligands, we synthesized thirteen 3-{4-(2-aminoethoxy)phenyl}propanoic acid derivatives, which are designed based on the structures of rosiglitazone and 15d-PGJ2. Among these compounds, compound 9 was found to be as potent as rosiglitazone in a binding assay and a preadipocyte differentiation test. Molecular modeling suggested that the nonyl group of 9 interacted with hydrophobic amino acid residues constructing the hydrophobic region of PPARγ protein where the alkyl chain of 15d-PGJ2 is expected to be located.
