The synthesis of cis-N-benzyl-3-methylamino-4-methylpiperidine (5) via hydroboration of tetrahydropyridine 3 followed by oxidation and reductive amination was optimized and scaled up to produce 10-kg quantities of product. Three routes to 3 were identified, and the reduction of pyridinium salt 7 was selected as the most preferable to run on-scale. The hydroboration and oxidative workup were carefully studied to optimize throughput on that transformation, as was the reductive amination.
DHB Ripin合作论文数1christian koecher合作论文数1BLUMENKOPF TODD ANDREW合作论文数1Mark E Flanagan合作论文数1Jl Doty合作论文数1Kees Pouwer合作论文数1Jianmin Sun合作论文数1John J. Teixeira合作论文数1
Weiling Cai合作论文数China University of Mining and Technology, China Univ. of Mining and Technol.1Klaus W. Laue合作论文数1Glenn Wilcox合作论文数1Cliff Meltz合作论文数1Jeffery M. Casavant合作论文数1Ton R. Vries合作论文数1
