Zhang Xingxian
2012
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Journal
Chinese Journal of Pharmaceuticals
Abstract
Methyl(3S)-3-(tert-butoxycarbonylamino)-4-oxobutanoate,an important chiral intermediate of sitagliptin,was synthesized from L-aspartic acid by selective methylation in the presence of SOCl2 to give 4-methyl L-aspartate hydrochloride,which was subjected to Boc-protection,acylation with ethyl chloroformate and reduction by NaBH4,followed by oxidization by NaClO/TEMPO with an overall yield of about 41%.