| Pharmaceutical intermediate is the basis for the pharmaceutical industry. In the paper, two important pharmaceutical intermediates 2-(4-bromophenoxy)-N,N-dimethylethylamine and 2-amino-3-(3-(5-benzyloxy)-1H-indol)-propionic acid were synthesized. And the optimized synthesis processes were proposed.Tamoxifen is the leading therapeutic agent for the treatment of estrogen-dependent breast cancer and other emerging clinical applications.2-(4-bromophenoxy)-N,N-dimethylethylamine is an important side chain of Tamoxifen, so research on synthesis of 2-(4-bromophenoxy)-N,N-dimethylethylamine is of great significance both in theoretical and practical side.2-(4-bromophenoxy)-N,N-dimethylethylamine was synthesized by 4-bromophenol and 2-dimethylaminoethyl chloride hydrochloride by Williamson etherification. General yield was 86.4% with good purity, which is more than 96%. Final product was characterized by IR spectrometer and 1H-NMR. Much work has been done in the optimization of synthesis process. The optimum process with high yield achieved in the study is stable, green and easy to operate.2-amino-3-(3-(5-benzyloxy)-1H-indol)-propionic acid is the important inter-mediate of 5-hydroxytryptophan (5-HTP).5-HTP is one of the essential amino acids, the additives of feed, food, pharmaceutical. The current mainstream production process is to extract from Ghana seeds. However, developing an efficient chemical synthesis route is urgent because of market demand. So research on synthesis of 2-amino-3-(3-(5-benzyloxy)-1H-indol)-propionic acid is of great significance both in theoretical and practical side. It was synthesized using 4-nitro-phenol as raw material by etherification, reduction, nitrification, reduction, condensation, cyclization, hydrolysis, decarboxylation, rehydrolysis and other processes in the paper. General yield is 42.4% with good purity. Final product was characterized by IR spectrometer and 1H-NMR. |
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