Reaktion #2447713

Reaktionsgleichung

1-methyl-7-[4-(1-methyl-pyrrolidine-2-carbonyl)-piperazin-1-ylmethyl]-1H-indole-2-carboxylic acid-(3-amino-5-tert-butyl-2-methoxy-phenyl)-amide trihydrochloride

propylsulphonic acid chloride

triethylamine

propylsulphonic acid chloride

pyridine

→

(S)-1-methyl-7-[4-(1-methyl-pyrrolidine-2-carbonyl)-piperazin-1-ylmethyl]-1H-indole-2-carboxylic acid-[5-tert-butyl-2-methoxy-3-(propane-1-sulphonylamino)-phenyl]-amide

Lösungsmittel

dichloromethane

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.STIRRINGthe mixture is stirred for a further 12 hours
2. 2
   Sonstigethe residue is purified by preparative HPLC (method 3)

Vorschrift

200 mg of 1-methyl-7-[4-(1-methyl-pyrrolidine-2-carbonyl)-piperazin-1-ylmethyl]-1H-indole-2-carboxylic acid-(3-amino-5-tert-butyl-2-methoxy-phenyl)-amide trihydrochloride are dissolved in 2 ml dichloromethane and mixed successively with 210 μl triethylamine, 80 μl propylsulphonic acid chloride and 70 μl pyridine. The mixture is stirred for 2 hours at ambient temperature, a further 80 μl of propylsulphonic acid chloride are added and the mixture is stirred for a further 12 hours. The solvents are eliminated in vacuo and the residue is purified by preparative HPLC (method 3).

Quelle