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
Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in va...Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in vacuum afforded thalidomide 1 and its corresponding derivatives 2—5 directly in yields 24%47%. Among them, compound 4 is the material in the synthesis of 3-amino and 3-amino-3′-fluoro substituted thalidomide. Compared with traditional methods, this method is more direct and convenient.展开更多
PMR(Polymerization of Monomer Reactants)型聚酰亚胺树脂(PI)以其优异的耐热氧化性能、机械性能、介电性能、良好的耐溶剂性能以及高的玻璃化转变温度,在航空、航天等领域得到了广泛的应用,并已成为目前使用最广泛的聚酰亚胺复合材料...PMR(Polymerization of Monomer Reactants)型聚酰亚胺树脂(PI)以其优异的耐热氧化性能、机械性能、介电性能、良好的耐溶剂性能以及高的玻璃化转变温度,在航空、航天等领域得到了广泛的应用,并已成为目前使用最广泛的聚酰亚胺复合材料的基体树脂[1～3].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.
文摘Thalidomide and its derivatives have great potentials in immune therapy. This research note presented that heating the mixture of phthalic anhydride or its chloro or nitro substituted derivatives and L-glutamine in vacuum afforded thalidomide 1 and its corresponding derivatives 2—5 directly in yields 24%47%. Among them, compound 4 is the material in the synthesis of 3-amino and 3-amino-3′-fluoro substituted thalidomide. Compared with traditional methods, this method is more direct and convenient.
