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Synthetic scheme for generating (S)-2-amino-4-(3-methylguanidino)butanoic acid analogues. Reagents and Conditions: (i) DEAD, PPh3, THF, 0 °C-RT, 3–16 h; (ii) DIPEA, CH3CN, RT, 24 h; (iii) 4M HCl/1,4-dioxane, RT, 24–72 h, 12%–67% overall; (iv) SOCl2, 0 °C for 30 min, reflux for 1 h, RT overnight, 44%–84%. Adapted with permission from [112]. Copyright 2005 American Chemical Society.
