476003-32-4Relevant academic research and scientific papers
Synthesis and binding affinities of fluoroalkylated raloxifenes
Lee, Kyo Chul,Moon, Byung Seok,Lee, Jae Hak,Chung, Kyoo-Hyun,Katzenellenbogen, John A.,Chi, Dae Yoon
, p. 3649 - 3658 (2007/10/03)
Three fluoroalkylated derivatives (1-3) of the selective estrogen receptor modulator (SERM), raloxifene, have been synthesized. The key step in the synthesis is the C-C bond formation of benzo[b]thiophene and a substituted phenyl group (ring C) using a Stille reaction. The in vitro binding affinities of the substituted raloxifenes 1-3 are 45, 60, 89%, respectively, relative to the affinity of estradiol, which is higher than the affinity of raloxifene itself (25%). When labeled with the positron-emitting radionuclide, these compounds might be useful as PET imaging agents for estrogen receptor-positive breast tumors.
Total synthesis of both enantiomers of dictyochromenol and their (Z)-isomers.
Aoki, Kota,Takahashi, Mihoko,Hashimoto, Masaru,Okuno, Toshikatsu,Kurata, Kazuya,Suzuki, Minoru
, p. 1915 - 1924 (2007/10/03)
Total syntheses of both enantiomers of dictyochromenol (1) and its (Z)-stereoisomer (2) were achieved with high enantiomeric purity. The results of this study reveal the relationship between the optical rotation of the resolved 1 enantiomers.
