4,4-disubstituted-2-aminomethyl oxetanes are useful building blocks in medicinal chemistry. Previously they were prepared from the corresponding hydroxylmethyl oxetanes in our lab, whose syntheses were plagued by use of organotin reagent and presence of tetrahydrofuran impurity. We have hence developed an improved synthesis of those compounds. In our approach, intermediate expoxide <b>3</b> was opened with dibenzylamine instead, and the resultant diol was then converted to oxetanes in good overall yield.

Improved synthesis of 4,4-disubstituted-2-aminomethyl oxetanes

2019 Fall National Meeting

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