反应详情

To a solution of 2-[3-(4-chlorobenzyl)-8-aza-bicyclo[3.2.1]oct-8-yl]-1-methyl-ethylamine in CH2Cl2 was added 3,4,5-trimethoxyphenylisocyanate at −78° C. After the addition, it was allowed to warm up to rt where it was stirred for 4 h. It was then diluted with CH2Cl2. The organic layer was washed with NaCl (sat.) and dried over Na2SO4. The crude product was purified on a silica-gel column with 3% (10% iPr-NH2 in MeOH) in EtOAc to give 55% of Example 4 (m.p. 115–120° C., M+: 502).

1. additionAfter the addition, it
2. washThe organic layer was washed with NaCl (sat.)
3. dry with materialdried over Na2SO4
4. customThe crude product was purified on a silica-gel column with 3% (10% iPr-NH2 in MeOH) in EtOAc