摘要
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.
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.
出处
《高等学校化学学报》
SCIE
EI
CAS
CSCD
北大核心
2007年第12期2330-2332,共3页
Chemical Journal of Chinese Universities
