1-Methylindole-2-sulfonyl chloride → 4-[3-Methanesulfonyl-4-(1-methyl-1H-indole-2-sulfonylamino)-phenyl]-piperidine-1-carboxylic acid tert-butyl ester

関与物質

反応条件

反応手順

To a solution of 4-(4-amino-3-methanesulfonyl-phenyl)-piperidine-1-carboxylic acid tert-butyl ester (cf. Example 20e, 0.050 g) in dichloromethane (2.0 ml) was added 1-methyl-1H-indole-2-sulfonyl chloride (0.036 g; cf. Chan, Ming Fai; Wu, Chengde; Raju, Bore Gowda; Kogan, Timothy; Kois, Adam; Verner, Erik Joel; Castillo, Rosario Silvestre; Yalamorri, Venkatachalapathi; Balaji, Vitukudi Narayanaiyengar, U.S. Pat. No. 5,962,490) and DMAP (0.021 g). The reaction mixture was stirred at 80° C. for 18 h, cooled and directly chromatographed on silica gel using heptane/ethyl acetate as eluent to obtain the title compound (0.048 g) as a yellowish foam. MS (ISN): 546.5 (M−H)−

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