Reaktion #476864

Reaktionsgleichung

4-(2-Methyl-thiazol-4-yl)-benzenesulfonyl chloride

Intermediate 90

5-Chloro-thiophene-2-carboxylic acid [(S)-2-amino-3-(4-methyl-piperazin-1-yl)-3-oxo-propyl]-amide dihydrochloride

→

5-Chloro-thiophene-2-carboxylic acid {(S)-3-(4-methyl-piperazin-1-yl)-2-[4-(2-methyl-thiazol-4-yl)-benzenesulfonylamino]-3-oxo-propyl}-amide hydrochloride

Lösungsmittel

DCM

DCM

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThen the solution was evaporated to dryness
2. 2
   Sonstigepurified by silica gel chromatography
3. 3
   workup.DISSOLUTIONThe compound was dissolved in DCM
4. 4
   workup.ADDITIONHCl (2 M in diethyl ether (500 ml)) was added
5. 5
   Sonstigethe solvents were evaporated to dryness

Vorschrift

Intermediate 90 (0.2 g, 0.5 mmol) was dissolved in 10 ml DCM and TEA (0.35 ml, 2.5 mmol). Commercially available 4-(2-Methyl-thiazol-4-yl)-benzenesulfonyl chloride (130 mg, 0.47 mmol) in 5 ml DCM was slowly added at 0° C. and the reaction was stirred for 16 h. Then the solution was evaporated to dryness and purified by silica gel chromatography. The compound was dissolved in DCM, HCl (2 M in diethyl ether (500 ml)) was added and the solvents were evaporated to dryness.

Quelle