5665-20-3Relevant academic research and scientific papers
Enantioselective α-Benzylation of Acyclic Esters Using π-Extended Electrophiles
Schwarz, Kevin J.,Yang, Chao,Fyfe, James W. B.,Snaddon, Thomas N.
supporting information, p. 12102 - 12105 (2018/09/11)
The first asymmetric cooperative Lewis base/palladium catalyzed benzylic alkylation of acyclic esters is reported. This reaction proceeds via stereodefined C1-ammonium enolate nucleophiles. Critical to its success was the identification of benzylic phosphate electrophiles, which were uniquely reactive. Alkylated products were obtained with very high levels of enantioselectivity, and this method has been applied toward the synthesis of the thrombin inhibitor DX-9065a.
Antihyperglycemic Activity of Novel Naphthalenyl 3H-1,2,3,5-Oxathiadiazole 2-Oxides
Ellingboe, John W.,Lombardo, Louis J.,Alessi, Thomas R.,Nguyen, Thomas T.,Guzzo, Frieda,et al.
, p. 2485 - 2493 (2007/10/02)
A series of naphthalenyl 3H-1,2,3,5-oxathiadiazole 2-oxides was prepared and tested for antihyperglycemic activity in the db/db mouse, a model for type 2 (non-insulin dependent) diabetes mellitus.Substitution at the 1-,5-, or 8-positions of the naphthalene ring with a halogen was found to be beneficial to antihyperglycemic activity. 4--3H-1,2,3,5-oxathiadiazole 2-oxide (45), one of the most potent compounds in this series, was selected for further pharmacological evaluation.
Synthesis of Naphthoquinolizidines - Analogs of Cryptopleurine
Mukerjee, Y. N.,Gaur, S. P.,Jain, P. C.,Anand, Nitya
, p. 985 - 987 (2007/10/02)
Condensation of the appropriate bromomethylnaphthalene (I) with 2-(1,3-dioxa-2-cyclopentyl)pyridine followed by treatment with 48percent HBr affords 3-methoxynaphthoquinolizinium bromide (8), 3-methoxy-(9)-, 2-methoxy-(10)- and 2,3-dimethoxy-(11)-naphthoquinolizinium bromides.The compounds (8-11) on catalytic hydrogenation over PtO2 give the corresponding naphthoquinolizidines (12-15).None of these compounds show any significant anticancer activity.
