So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Kinzel, Olaf; Alfieri, Anna; Altamura, Sergio; Brunetti, Mirko; Bufali, Simone; Colaceci, Fabrizio; Ferrigno, Federica; Filocamo, Gessica; Fonsi, Massimiliano; Gallinari, Paola; Malancona, Savina; Hernando, Jose Ignacio Martin; Monteagudo, Edith; Orsale, Maria Vittoria; Palumbi, Maria Cecilia; Pucci, Vincenzo; Rowley, Michael; Sasso, Romina; Scarpelli, Rita; Steinkuehler, Christian; Jones, Philip researched the compound: (S)-4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid( cas:138775-03-8 ).Safety of (S)-4-((Benzyloxy)carbonyl)-1-(tert-butoxycarbonyl)piperazine-2-carboxylic acid.They published the article 《Identification of MK-5710 ((8aS)-8a-methyl-1,3-dioxo-2-[(1S,2R)-2-phenylcyclo- propyl]-N-(1-phenyl-1H-pyrazol-5-yl)hexahydro-imidazo[1,5-a]pyrazine-7(1H)-carboxamide), a potent smoothened antagonist for use in Hedgehog pathway dependent malignancies, Part 2》 about this compound( cas:138775-03-8 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: MK5710 preparation Hedgehog signaling smoothened antagonist antitumor pharmacokinetics. We’ll tell you more about this compound (cas:138775-03-8).
The Hedgehog (Hh-) signaling pathway is a key developmental pathway which gets reactivated in many human tumors, and smoothened (Smo) antagonists are emerging as novel agents for the treatment of malignancies dependent on the Hh-pathway, with the most advanced compounds demonstrating encouraging results in initial clin. trials. A novel series of potent bicyclic hydantoin Smo antagonists was reported in the preceding article, these have been resolved, and optimized to identify potent homochiral derivatives with clean off-target profiles and good pharmacokinetic properties in preclin. species. While showing in vivo efficacy in mouse allograft models, unsubstituted bicyclic tetrahydroimidazo[1,5-a]pyrazine-1,3(2H,5H)-diones were shown to epimerize in plasma. Alkylation of the C-8 position blocks this epimerization, resulting in the identification of MK-5710 which was selected for further development.
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Reference:
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com