Cu(I)-catalyzed diamination of disubstituted terminal olefins: an approach to potent NK1 antagonist.
This paper describes a diamination process using di-tert-butyldiaziridinone as nitrogen source and CuCl as catalyst. A wide variety of disubstituted terminal olefins can be efficiently diaminated in good yields under mild condition. This diamination process was used to synthesize potent NK(1) antagonist Sch 425078.
Wen
Yuehong
Y
Department of Chemistry, Colorado State University, Fort Collins, Colorado 80523, USA.
Zhao
Baoguo
B
Shi
Yian
Y
D000475:Alkenes / Q000737:chemistry*; D001388:Aziridines / Q000737:chemistry*; D002384:Catalysis; D020650:Combinatorial Chemistry Techniques; D003300:Copper / Q000737:chemistry*; D007093:Imidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D064729:Neurokinin-1 Receptor Antagonists; D009584:Nitrogen / Q000737:chemistry
D000475:Alkenes; D001388:Aziridines; D007093:Imidazoles; D064729:Neurokinin-1 Receptor Antagonists; C541325:Sch 425078; C527442:di-tert-butyldiaziridinone; D003300:Copper; D009584:Nitrogen