Abstract To date, the synthesis of l-anserine has relied on the use of naturally occurring 1- methyl-l-histidine as a precursor, however its high cost prevents its use in the large-scale synthesis of l-anserine. With this in mind, we report herein a concise and efficient synthetic strategy, employing the 160-fold less expensive, l-histidine methyl ester dihydrochloride as a starting material, to afford the title compound in an overall yield of 88%, over four reaction ...