1411975-64-8Relevant academic research and scientific papers
A practical synthesis of (S)- tert -butyl 3-methyl-1,4-diazepane-1- carboxylate, the key intermediate of rho-kinase inhibitor K-115
Gomi, Noriaki,Kouketsu, Akiyasu,Ohgiya, Tadaaki,Shibuya, Kimiyuki
, p. 3171 - 3178 (2012/11/14)
A practical synthesis of (S)-tert-butyl 3-methyl-1,4-diazepane-1- carboxylate has been established for supplying this key intermediate of Rho-kinase inhibitor K-115 in a multikilogram production. The chiral 1,4-diazepane was constructed by intramolecular Fukuyama-Mitsunobu cyclization of a N-nosyl diamino alcohol starting from the commercially available (S)- or (R)-2-aminopropan-1-ol. In the same manner, an enantiomeric pair of a structural isomer were prepared for demonstration of the synthetic utility.
