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. 2018 Jun 15;23(6):1463. doi: 10.3390/molecules23061463

Scheme 4.

Scheme 4

Continuous solid-phase synthesis (SPS) of Mipsagargin (6). Reagents and conditions: (a) Fmoc-Glu-OtBu, DIPEA, DCM, 3 h; (b) Fmoc-Glu-OtBu, PyBOP, DIPEA, DMF, 16 h; (c) 20% piperidine–DMF, 2 × 20 min; (d) Boc-Asp(All)-OH, PyBOP, DIPEA, DMF, 18 h; (e) Me2NBH3 in DCM, Pd(PPh3)4 in DCM, 6 h; (f) 5, PyBOP, DIPEA, DCM, 18 h; (g) TFA–DCM (1:1 with a few drops of H2O added), 1 h; all reactions were carried out at rt.