As an important protective group of amines and amino acids,tert-butoxycarbonyl(Boc) group was extensively used in organic synthesis.Though many mild and selective reagents could be used,there is still a need for the d...As an important protective group of amines and amino acids,tert-butoxycarbonyl(Boc) group was extensively used in organic synthesis.Though many mild and selective reagents could be used,there is still a need for the development of a more simple and convenient method for deprotection.In this paper,a new method for the deprotection of N-Boc group with silica gel in refluxing toluene was reported.The reactions were mostly achieved in 5 h with high yields(75%-98%).N-Boc protected indoline and benzylamine,which are not deprotected with other mild method,could be deprotected with our method in good yields(89% and 95%,respectively).Additionally the deprotection of other carbamates such as Cbz,Fmoc and ethyl carbamate wasn′t observed under same conditions.展开更多
文摘As an important protective group of amines and amino acids,tert-butoxycarbonyl(Boc) group was extensively used in organic synthesis.Though many mild and selective reagents could be used,there is still a need for the development of a more simple and convenient method for deprotection.In this paper,a new method for the deprotection of N-Boc group with silica gel in refluxing toluene was reported.The reactions were mostly achieved in 5 h with high yields(75%-98%).N-Boc protected indoline and benzylamine,which are not deprotected with other mild method,could be deprotected with our method in good yields(89% and 95%,respectively).Additionally the deprotection of other carbamates such as Cbz,Fmoc and ethyl carbamate wasn′t observed under same conditions.
