1.1: dichloromethane / 2 h / 25 °C 2.1: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 24 h / 25 °C 3.1: Grubb's 2nd generation catalyst / toluene / 4 h / 110 °C 3.2: 20 °C View Scheme

1: (-)-10-CSA / chloroform; methanol 2: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine / dichloromethane / 20 °C 3: piperidine / N,N-dimethyl-formamide / 0.33 h / 20 °C 4: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; 1,2-dichloro-ethane / dichloromethane / 20 °C 5: trifluoroacetic acid; 2-[(2-Hydroxy-1,1-bis[hydroxymethyl]ethyl)amino]ethanesulfonic acid / dichloromethane / 2 h 6: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 48 h / 20 °C View Scheme

1: 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine / dichloromethane / 20 °C 2: piperidine / N,N-dimethyl-formamide / 0.33 h / 20 °C 3: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; 1,2-dichloro-ethane / dichloromethane / 20 °C 4: trifluoroacetic acid; 2-[(2-Hydroxy-1,1-bis[hydroxymethyl]ethyl)amino]ethanesulfonic acid / dichloromethane / 2 h 5: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 48 h / 20 °C View Scheme

1: piperidine / N,N-dimethyl-formamide / 0.33 h / 20 °C 2: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; 1,2-dichloro-ethane / dichloromethane / 20 °C 3: trifluoroacetic acid; 2-[(2-Hydroxy-1,1-bis[hydroxymethyl]ethyl)amino]ethanesulfonic acid / dichloromethane / 2 h 4: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 48 h / 20 °C View Scheme

1: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; 1,2-dichloro-ethane / dichloromethane / 20 °C 2: trifluoroacetic acid; 2-[(2-Hydroxy-1,1-bis[hydroxymethyl]ethyl)amino]ethanesulfonic acid / dichloromethane / 2 h 3: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 48 h / 20 °C View Scheme

1: trifluoroacetic acid; 2-[(2-Hydroxy-1,1-bis[hydroxymethyl]ethyl)amino]ethanesulfonic acid / dichloromethane / 2 h 2: 1-hydroxy-7-aza-benzotriazole; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane / 48 h / 20 °C View Scheme

1.1: benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / dichloromethane / 0.17 h / 0 °C 1.2: 0 - 20 °C 2.1: trifluoroacetic acid / dichloromethane / 0 - 20 °C 3.1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane; acetonitrile 4.1: triethylsilane; trifluoroacetic anhydride / 2 h / 0 - 20 °C 5.1: triethylamine / dichloromethane / 3 h / 0 - 20 °C View Scheme

1: triethylsilane; trifluoroacetic anhydride / 2 h / 0 - 20 °C 2: triethylamine / dichloromethane / 3 h / 0 - 20 °C View Scheme

1.1: benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride; N-ethyl-N,N-diisopropylamine / tetrahydrofuran; dichloromethane / 0.17 h 2.1: triethylamine; trifluoroacetic anhydride / dichloromethane / 0 °C 3.1: sodium hydrogencarbonate / methanol / 2 h / 70 °C / pH 6 / aq. phosphate buffer 4.1: benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / dichloromethane / 0.17 h / 0 °C 4.2: 0 - 20 °C 5.1: trifluoroacetic acid / dichloromethane / 0 - 20 °C 6.1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane; acetonitrile 7.1: triethylsilane; trifluoroacetic anhydride / 2 h / 0 - 20 °C 8.1: triethylamine / dichloromethane / 3 h / 0 - 20 °C View Scheme

1.1: triethylamine; trifluoroacetic anhydride / dichloromethane / 0 °C 2.1: sodium hydrogencarbonate / methanol / 2 h / 70 °C / pH 6 / aq. phosphate buffer 3.1: benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate; N-ethyl-N,N-diisopropylamine / dichloromethane / 0.17 h / 0 °C 3.2: 0 - 20 °C 4.1: trifluoroacetic acid / dichloromethane / 0 - 20 °C 5.1: benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; HATU / dichloromethane; acetonitrile 6.1: triethylsilane; trifluoroacetic anhydride / 2 h / 0 - 20 °C 7.1: triethylamine / dichloromethane / 3 h / 0 - 20 °C View Scheme