4.2 Article

A practical synthesis of deuterated methylamine and dimethylamine

期刊

JOURNAL OF CHEMICAL RESEARCH
卷 45, 期 3-4, 页码 265-268

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SAGE PUBLICATIONS LTD
DOI: 10.1177/1747519820969636

关键词

deuterated drugs; deuteration; dimethylamine; methylamine; methylation

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A new method has been developed to prepare deuterated methylamine and dimethylamine, which offers relatively high yields and involves simple purifications, serving as a beneficial supplement for the development and synthesis of deuterated drugs in the future.
In recent years, several deuterated drugs have entered clinical trials and have been approved for use. Deuterated methylamine and dimethylamine as important intermediates play significant roles in the preparation of deuterated drugs. In this study, we have developed a new method to prepare deuterated methylamine and dimethylamine. This method employs Boc-benzylamine as the starting material and TsOCD3 as the deuterated methylation reagent. Our method gives relatively high yields and involves simple purifications, which provide a favourable supplement for the development and synthesis of deuterated drugs in the future.

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