

MF: C27H37ClN8O5
A method is described for the synthesis ...
Boc-D-Phe-Pip-Arg-pNA*HCl
2HCl*H-D-Phe-Pip-Arg-pNA
| Conditions | Yield |
|---|---|
|
With
hydrogenchloride;
In
ethyl acetate;
for 2h;
|
96% |
Boc-D-Phe-OH
2HCl*H-D-Phe-Pip-Arg-pNA
| Conditions | Yield |
|---|---|
|
Multi-step reaction with 5 steps
1: 85 percent / DCC, NMM, HOBt / dimethylformamide / 1.) 0 deg C, 1 h; 2.) r.t., 16 h
2: 65 percent / NH2NH2*H2O / methanol / 72 h / Ambient temperature
3: 2.6 M HCl, t-BuONO / dimethylformamide; ethyl acetate / 0.33 h / -25 °C
4: DIPEA / dimethylformamide; ethyl acetate / 4 °C
5: 96 percent / 2.6 M HCl / ethyl acetate / 2 h
With
4-methyl-morpholine; hydrogenchloride; tert.-butylnitrite; benzotriazol-1-ol; hydrazine hydrate; N-ethyl-N,N-diisopropylamine; dicyclohexyl-carbodiimide;
In
methanol; ethyl acetate; N,N-dimethyl-formamide;
|
Boc-D-Phe-OH
(S)-methyl pipecolinate hydrochloride
Boc-D-Phe-Pip-OMe
Boc-D-Phe-Pip-N2H3