145920-52-1Relevant articles and documents
Synthesis of Chiral cis-Cyclopropane Bearing Indole and Chromone as Potential TNFα Inhibitors
Kanada, Ryutaro,Tanabe, Makoto,Muromoto, Ryuta,Sato, Yukina,Kuwahara, Tomoki,Fukuda, Hayato,Arisawa, Mitsuhiro,Matsuda, Tadashi,Watanabe, Mizuki,Shuto, Satoshi
, p. 7672 - 7682 (2018)
Conformationally restricted analogues of SPD-304, the first small-molecule TNFα inhibitor, in which two heteroaryl groups, indole and chromone, are connected by chiral methyl- or ethyl-cis-cyclopropane, were designed. Synthesis of these molecules was achieved via Suzuki-Miyaura or Stille coupling reactions with chiral bromomethylenecyclopropane or iodovinyl-cis-cyclopropane as the substrate, both of which were prepared from chiral methylenecyclopropane as a common intermediate, constructing the heteroaryl-methyl or -ethyl-cis-cyclopropane structures as key steps. This study presents an efficient synthesis of a series of chiral cis-cyclopropane conjugates with two heteroaryl groups.
Total synthesis of (-)-pseudolaric acid B
Trost, Barry M.,Waser, Jerome,Meyer, Arndt
supporting information; experimental part, p. 16424 - 16434 (2009/05/09)
We report a full account of our work toward the total synthesis of pseudolaric acid B (1a), a diterpene acid isolated from the bark of Pseudolarix kaempferi Gordon (pinaceae). Compound 1a is an antifungal and antifertility agent. Furthermore, its capacity
Asymmetric desymmetrization based on an intramolecular haloetherification: A highly effective and recyclable chiral nonracemic auxiliary, 2-exo-methyl-3-endo-phenyl-5-norbornene-2-carboxaldehyde, for meso-1,3- and meso-1,4-diols
Fujioka, Hiromichi,Fujita, Tetsuya,Kotoku, Naoyuki,Ohba, Yusuke,Nagatomi, Yasushi,Hiramatsu, Atsushi,Kita, Yasuyuki
, p. 5386 - 5397 (2007/10/03)
A new chiral auxiliary, a 3-endo-phenyl norbornene aldehyde derivative, which is a crystalline, very stable, and easily handled, was developed for the desymmetrization of meso-1,3- and meso-1,4-diols. The key step of the method, an intramolecular bromoeth
