反应详情

26.6 g of BOP, 13.6 g of 1-(carbobenzyloxy)-2-piperidinecarboxylic acid and then 11.9 ml of triethylamine are added, at 0° C., to a solution of 8 g of 1-Boc-piperazine in 80 ml of acetonitrile. The medium is stirred at AT for 12 hours and then concentrated. The medium is taken up in EtOAc, and washed three times with a saturated Na2CO3 solution and then with a saturated NaCl solution. After drying over MgSO4 and evaporation, 35.45 g of reaction crude are recovered. It is taken up in DCM and then washed twice with 5M sodium hydroxide, and with a saturated NaCl solution, and then dried over MgSO4. After evaporation, the solid is triturated in TBME, filtered, rinsed with TBME, and then dried, to give 17.93 g of the desired compound.

1. concentrationconcentrated
2. washwashed three times with a saturated Na2CO3 solution
3. dry with materialAfter drying over MgSO4 and evaporation, 35.45 g of reaction crude
4. customare recovered
5. washwashed twice with 5M sodium hydroxide
6. dry with materialwith a saturated NaCl solution, and then dried over MgSO4
7. customAfter evaporation
8. customthe solid is triturated in TBME
9. filtrationfiltered
10. washrinsed with TBME
11. customdried