98601-72-0Relevant academic research and scientific papers
Organocatalytic Atroposelective Friedl?nder Quinoline Heteroannulation
Shao, You-Dong,Dong, Meng-Meng,Wang, You-An,Cheng, Pei-Ming,Wang, Tao,Cheng, Dao-Juan
, p. 4831 - 4836 (2019)
An atroposelective Friedl?nder heteroannulation reaction of 2-aminoaryl ketones with α-methylene carbonyl derivatives has been developed for the first time with chiral phosphoric acid as an efficient organocatalyst. The desired enantioenriched axially chi
Palladium-Catalyzed Cascade Reductive and Carbonylative Cyclization of Ortho-Iodo-Tethered Methylenecyclopropanes (MCPs) Using N-Formylsaccharin as CO Source
Fan, Xing,Shi, Min,Wei, Yin
supporting information, p. 5677 - 5683 (2019/11/16)
A palladium-catalyzed reductive and carbonylative cyclization of ortho-iodo-tethered methylenecyclopropanes (MCPs) using N-formylsaccharin as CO source has been developed, affording the desired indanone derivatives in moderate to good yields with high regio- and stereoselectivity and good functional group compatibility.
Novel 4,1-benzoxazepine derivatives with potent squalene synthase inhibitory activities
Miki, Takashi,Kori, Masakuni,Mabuchi, Hiroshi,Banno, Hiroshi,Tozawa, Ryu-ichi,Nakamura, Masahira,Itokawa, Shigekazu,Sugiyama, Yasuo,Yukimasa, Hidefumi
, p. 401 - 414 (2007/10/03)
A series of (3,5-trans)-2-oxo-5-phenyl-1,2,3,5-tetrahydro-4,1-benzoxazepine derivatives were synthesized and evaluated for squalene synthase inhibitory and cholesterol biosynthesis inhibitory activities. Through modification of substituents of the lead compounds 1a and 1b, it was found that 4,1-benzoxazepine-3-acetic acid derivatives with isobutyl and neopentyl groups at the 1-position, the chloro atom at the 7-position, and the chloro and methoxy groups at the 2'-position on the 5-phenyl ring, had potent squalene synthase inhibitory activity. Among such compounds, the 5-(2,3-dimethoxyphenyl) derivative 2t exhibited potent inhibition of cholesterol biosynthesis in HepG2 cells. As a result of optical resolution study of 2t, the absolute stereochemistry required for inibitory activity was determined to be 3R,5S. In vivo study showed that the sodium salt of (3R,5S)-7-chloro-5-(2,3-dimethoxyphenyl)-1-neopentyl-2-oxo-1,2,3,5-tetrahydro-4,1-benzoxazepine-3-aceitc acid 20 effectively reduced plasma cholesterol in marmosets. Copyright
