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Scheme 3 | EJNMMI Research

Scheme 3

From: In vivo evaluation of two tissue transglutaminase PET tracers in an orthotopic tumour xenograft model

Scheme 3

Synthesis of ERW1041E. Reagents and conditions: (i) hydroxylamine hydrochloride, H2O, 2 h, room temperature (rt), then NaHCO3, Br2, 16 h, 0 °C to rt, 52%; (ii) allylamine hydrochloride, KHCO3, H2O, 3 h, rt, 50%; (iii) LiBH4, ethanol/THF, 2 h, − 80 °C, then CDI, MeCN, 2 h, rt, 78%; (iv) proline methyl ester hydrochloride, DiPEA, DCM/DMF, 16 h, rt, 60%; (v) NaOH, dioxane/MeOH/H2O, 2 h, rt, 89%; (vi) amine 4, EDC, HOBt, N-methylmorpholine, DMF, 2 h, rt, 96%

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