Cl.C(OC([N:9]1[CH2:13][CH2:12][CH2:11][C@@H:10]1[CH2:14][N:15]([CH2:52][C:53]1[CH:58]=[CH:57][C:56]([F:59])=[CH:55][CH:54]=1)[CH2:16][C:17]1[CH:22]=[C:21]([C:23]2[CH:50]=[CH:49][C:26]3[N:27](C(C4C=CC=CC=4)(C4C=CC=CC=4)C4C=CC=CC=4)[N:28]=[N:29][C:25]=3[CH:24]=2)[CH:20]=[CH:19][C:18]=1[F:51])=O)(C)(C)C>O1CCOCC1.CO>[NH:27]1[C:26]2[CH:49]=[CH:50][C:23]([C:21]3[CH:20]=[CH:19][C:18]([F:51])=[C:17]([CH:22]=3)[CH2:16][N:15]([CH2:52][C:53]3[CH:58]=[CH:57][C:56]([F:59])=[CH:55][CH:54]=3)[CH2:14][C@H:10]3[CH2:11][CH2:12][CH2:13][NH:9]3)=[CH:24][C:25]=2[N:29]=[N:28]1A solution of hydrochloric acid in dioxane (4M, 2 mL) was added to a solution of (R)-2-({(4-fluoro-benzyl)-[2-fluoro-5-(1-trityl-1H-benzotriazol-5-yl)-benzyl]-amino}-methyl)-pyrrolidine-1-carboxylic acid tert-butyl ester (119 mg, 0.15 mmol) in 5 mL of methanol and the resulting solution stirred at ambient temperature for 24 h. The volatiles were removed in vacuo and purified by HPLC. The product obtained was treated with hydrochloric acid to give 40 mg of product. LC/MS (long run): Retention time, 6.20 min; (M+H)=433.
Wird geladen…