10004-42-9Relevant articles and documents
METHOD FOR PRODUCING IODOOXAZOLE COMPOUND, AND METHOD FOR PRODUCING OXAZOLE COMPOUND
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Paragraph 0043-0045, (2021/09/15)
PROBLEM TO BE SOLVED: To produce an iodooxazole compound inexpensively and safely without using oxidizing agents. SOLUTION: On the basis of the following chemical formula (1) an iminoether compound and an iodinating agent are mixed and reacted with each other with light irradiation, to produce an iodooxazole compound. In the formula (1), R1, R2 each denote an aromatic group. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT
A novel synthetic method of 2,4-disubstituted oxazoles using carboxylic acid-derived Bu2Sn[OC(O)R]2
Yoneyama, Hiroki,Oka, Naoki,Usami, Yoshihide,Harusawa, Shinya
supporting information, (2020/05/21)
A novel synthetic method for the preparation of 2,4-disubstituted oxazoles was developed, entailing the reaction of dibutyltin diacylates Bu2Sn[OC(O)R]2 with 1-substituted acetylenes and TMSN3 to afford a range of 2,4-disu
Discovery of amide replacements that improve activity and metabolic stability of a bis-amide smoothened antagonist hit
Brown, Matthew L.,Aaron, Wade,Austin, Richard J.,Chong, Angela,Huang, Tom,Jiang, Ben,Kaizerman, Jacob A.,Lee, Gary,Lucas, Brian S.,McMinn, Dustin L.,Orf, Jessica,Rong, Minqing,Toteva, Maria M.,Xu, Guifen,Ye, Qiuping,Zhong, Wendy,Degraffenreid, Michael R.,Wickramasinghe, Dineli,Powers, Jay P.,Hungate, Randall,Johnson, Michael G.
scheme or table, p. 5206 - 5209 (2011/10/09)
A bis-amide antagonist of Smoothened, a seven-transmembrane receptor in the Hedgehog signaling pathway, was discovered via high throughput screening. In vitro and in vivo experiments demonstrated that the bis-amide was susceptible to N-acyl transferase mediated amide scission. Several bioisosteric replacements of the labile amide that maintained in vitro potency were identified and shown to be metabolically stable in vitro and in vivo.