Study On The Synthesis And Technology Of The Tert-Butyl Carbazate

In the synthetic methodology, the method to protect groups is one of the most important and necessary strategy, it also carried out in organic chemistry. Especially in the last decade years, the new protective group had been widely used in organic synthesis and transformation of natural products, e.g., carbohydrates, proteins, alkaloids, new pesticides and new medicine, and achieved great success. In this paper, synthesis of tert-Butyl carbazate has been discussed. BOC-hydrazide is a new amino-protecting group, and do not decompose under rigorous conditions, such as in the catalytic hydrogenation and nucleophilic reaction. Tert-butyl carbazate has been widely used as amino-protection group in protein synthesis of peptide; in addition, tert-Butyl carbazate is applied to synthesis anti-cancer drug intermediates in the pharmaceutical industry.The experiments are made up of three parts: first, the elimination reaction of tert-butanol and phenyl chloroformate for prepare the t-Butyl phenyl carbonate using the quinoline as the acid binding agents. In part two, synthesis of t-Butyl carbazate by the substitution reaction of phenyl chloroformate with hydrazine hydrate. Part three, the optimizations of producing technology have also been studied.There are have some advantages in this paper: First, tert-Butyl carbazate, this method prepared have high purity, not easy to liquefied and almost do not have phenol; second, the process to synthesis tert-butyl phenyl carbonate reduce the energy consumption; third, the quinoline can be recovered and used many times, this technology also have advantage at mild conditions, lowed the cost and obtained phenol, it can be industrial produced convenient.