Reaktion #1611451

Reaktionsgleichung

trifluoroacetic acid

((S)-2-{3-[(4-cyano-phenylcarbamoyl)-methoxy]-benzoylamino}-4,5,6,7-tetrahydro-benzothiazol-6-yl)-carbamic acid tert-butyl ester

→

title compound

Ausbeute 60.2%

N—((S)-6-amino-4,5,6,7-tetrahydro-benzothiazol-2-yl)-3-[(4-cyano-phenylcarbamoyl)-methoxy]-benzamide

Ausbeute 60.2%

Lösungsmittel

methylene chloride

Reaktionsbedingungen

Aufarbeitung

1. 1
   Einengenthen concentrate under reduced pressure
2. 2
   SonstigePurify the residue by preparative reverse phase

Vorschrift

Add trifluoroacetic acid (1.0 mL, 14 mmol) to a solution of ((S)-2-{3-[(4-cyano-phenylcarbamoyl)-methoxy]-benzoylamino}-4,5,6,7-tetrahydro-benzothiazol-6-yl)-carbamic acid tert-butyl ester (0.14 g, 0.26 mmol) in methylene chloride (10 mL). Stir the mixture at room temperature for 15 h then concentrate under reduced pressure. Purify the residue by preparative reverse phase HPLC using acetonitrile/water with 0.1% trifluoroacetic acid additive as the eluent to provide 0.07 g of the title compound as a white powder. MS, electrospray 448.75 (M+H), rt. 1.21 min.

Quelle