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. Author manuscript; available in PMC: 2017 Sep 21.
Published in final edited form as: Bioconjug Chem. 2016 Sep 2;27(9):2157–2165. doi: 10.1021/acs.bioconjchem.6b00374

Scheme 2.

Scheme 2

Synthesis of NK1RL-Lys Linker, 4. Reagents and conditions: (a) (i) DCM, DMF wash, (ii) Fmoc-Asp(OtBu)-OH, PyBOP, DIPEA, DMF, 4 h; (b) (i) 20% piperidine in DMF, 3×10 min, (ii) Fmoc-Arg(pbf)-OH, PyBOP, DIPEA, DMF, 4 h; (c) (i) 20% piperidine in DMF, 3×10 min, (ii) Fmoc-PEG2-OH, PyBOP, DIPEA, DMF, 4 h; (d) L-733 060-AcOH, PyBOP, DIPEA, DMF, 12 h (e) TFA:H2O:TIPS, 95:2.5:25, 3×15 min, 26 %.