[N:1]1([CH2:6][C:7]2[CH:12]=[CH:11][C:10]([C:13]3[CH:17]=[C:16]([CH2:18][CH:19]([CH3:21])[CH3:20])[S:15][C:14]=3[S:22]([NH:25]C(C)(C)C)(=[O:24])=[O:23])=[CH:9][CH:8]=2)[CH:5]=[N:4][CH:3]=[N:2]1.B(Cl)(Cl)Cl>ClCCl>[N:1]1([CH2:6][C:7]2[CH:12]=[CH:11][C:10]([C:13]3[CH:17]=[C:16]([CH2:18][CH:19]([CH3:21])[CH3:20])[S:15][C:14]=3[S:22]([NH2:25])(=[O:23])=[O:24])=[CH:9][CH:8]=2)[CH:5]=[N:4][CH:3]=[N:2]13-(4-[1,2,4]Triazol-1-ylmethylphenyl)-5-iso-butyl-N-tert-butylthiophene-2-sulfonamide (146.4 mg, 0.34 mmol, see step (b) above) was mixed with BCl3 (1M solution in hexane) (2 mL, 1.7 mmol) in 5 mL of dichloromethane at rt and stirred for 1 h. The reaction mixture was extracted with ethyl acetate and water and subsequently dried over K2CO3. The solvent was evaporated and the resultant product was sufficiently pure to be used directly in the next step.
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