1.1: benzotriazol-1-ol; 4-methyl-morpholine; N'-(3-dimethylaminopropyl)-N-ethylcarbodiimide / acetonitrile; water / 5 h / 5 - 40 °C / Industry scale 2.1: sodium hydroxide; water / 2-methyl tetrahydrofuran / 7 h / 20 - 60 °C / Industry scale 2.2: 0.17 h / 20 - 30 °C / pH 1.5 - 3 / Industry scale View Scheme

1.1: benzotriazol-1-ol; 4-methyl-morpholine; N'-(3-dimethylaminopropyl)-N-ethylcarbodiimide / acetonitrile; water / 5 h / 5 - 40 °C / Industry scale 2.1: sodium hydroxide; water / 2-methyl tetrahydrofuran / 7 h / 20 - 60 °C / Industry scale 2.2: 0.17 h / 20 - 30 °C / pH 1.5 - 3 / Industry scale 3.1: N-ethyl-N,N-diisopropylamine; benzotriazol-1-ol; N'-(3-dimethylaminopropyl)-N-ethylcarbodiimide / ethyl acetate; acetonitrile; water / -5 - 30 °C / Industry scale 4.1: sodium acetate; sodium hypochlorite; acetic acid; 2,2,6,6-tetramethyl-1-piperidinyloxy, free radical / methyl acetate; water; tert-butyl methyl ether / 2 h / 5 - 15 °C / Industry scale View Scheme