172938-00-0Relevant articles and documents
Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat
Tran, Thuy-Anh,Shin, Young-Jun,Kramer, Bryan,Choi, Juyi,Zou, Ning,Vallar, Pureza,Martens, Peter,Douglas Boatman,Adams, John W.,Ramirez, Juan,Shi, Yunqing,Morgan, Michael,Unett, David J.,Chang, Steve,Shu, Hsin-Hui,Tung, Shiu-Feng,Semple, Graeme
, p. 1030 - 1035 (2015)
The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed in vivo activity after SC dosing in the monocrotaline model of PAH in rat.
A comparative study of thallium(iii) and iodine(iii)-mediated ring contraction reactions for the synthesis of indane
Khan, Ajmir,Silva, Luiz F.,Rabnawaz, Muhammad
supporting information, p. 2078 - 2084 (2021/02/06)
Reported herein is a comparative study of the synthesis of indaneviaring contraction reaction, mediated by iodine(iii) and thallium(iii). A series of protected 1,2-dihydronaphthalenes were synthesized and subjected to hydroxy(tosyloxy)iodobenzene (HTIB) and thallium(iii) nitrate trihydrate (TTN) in trimethyl orthoformate (TMOF) to compare the percent yields provided by both oxidizing agents. The yields of the ring contracted products (indanes) were in the range of 61-88% for reactions performed with TTN·3H2O in TMOF. However, the yields were found to be significantly lower (e.g., 18-34%) when using HTIB in TMOF with some addition products. This study provides an important development related to the efficacy of the two oxidizing agents for ring contraction reaction.
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: Orally active prostacyclin mimetics. Part 3
Hattori, Kouji,Tanaka, Akira,Okitsu, Osamu,Tabuchi, Seiichiro,Taniguchi, Kiyoshi,Nishio, Mie,Koyama, Satoshi,Higaki, Masahide,Seki, Jiro,Sakane, Kazuo
, p. 3091 - 3095 (2007/10/03)
The new classes of diphenylcarbamate derivatives with a tetrahydronaphthalene skeleton as highly potent and selective IP agonists have been discovered. The optimized diphenylcarbamate type compound FK-788: (R)-4 exhibited potent antiaggregative potency wi