反应详情

cis-2-(4-Fluoro-phenyl)-cyclopropyl-carbamic acid tert-butyl ester (0.239 g, 0.951 mmol) was dissolved in dichloromethane (5 ml). Under argon HCl (4 M in dioxan, 2.38 ml, 9.5 mmol) was added and the clear solution stirred at room temperature. After 3 hours a precipitate had formed and the reaction was complete according to tlc (30% EtOAc/cyclohexane) and LC/MS. The solvent was evaporated and the residue stirred with tBuOMe. The solid was filtered off and washed twice with tBuOMe and dried to yield 155 mg (87%) of the product as a white solid.

1. additionUnder argon HCl (4 M in dioxan, 2.38 ml, 9.5 mmol) was added
2. customAfter 3 hours a precipitate had formed
3. customThe solvent was evaporated
4. stirringthe residue stirred with tBuOMe
5. filtrationThe solid was filtered off
6. washwashed twice with tBuOMe
7. customdried