Hydrochloric Acid → (R)-N2-(Boc)-N5-(Cbz)-(R)-N-[2-hydroxy-1-(4-methoxyphenyl)ethyl]ornithine amide

Participants

Reaction Steps

Prepared according to the method described in Example 11(a) above from Nα -Boc-Nδ -Cbz-(R)-ornithine o-nitrophenyl ester (3.11 g; 6.38 mmol; see Example 4(a) above), (R)-4-methoxy-α-hydroxymethylbenzylamine hydrochloride (1.43 g; 7.02 mmol) and triethylamine (0.97 g; 9.57 mmol; instead of DiPEA) in CH2Cl2 (100 mL), 18 hours reaction time. The reaction mixture was submitted to aqueous work up using water, 1N HCl and brine, then dried, filtered and concentrated to give a yellow solid (3.69 g) which was used without purification.

Provenance & Evidence