Diisopropylamine → 4-(2-{6-[4-(2-Isopropylaminoethylamino)benzenesulfonyloxy]-benzothiazol-2-ylcarbamoyl}ethyl)piperidine-1-carboxylic acid tert-butyl ester

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Reaction Steps

According to the method of example 18, 4-(2-isopropylaminoethylamino)-benzenesulfonic acid 2-(3-piperid-4-ylpropionylamino)benzothiazol-6-yl ester hydrochloride is prepared by combining 4-{2-[6-(4-fluorobenzenesulfonyloxy)-benzothiazol-2-ylcarbamoyl]ethyl}piperidine-1-carboxylic acid tert-butyl ester (intermediate 23) with N,N-diisopropylamine. The compound obtained from the first step (4-(2-{6-[4-(2-isopropylaminoethylamino)benzenesulfonyloxy]-benzothiazol-2-ylcarbamoyl}ethyl)piperidine-1-carboxylic acid tert-butyl ester) is purified on a flash cartridge of 5 g of silica of porosity 15-35μ, with a gradient of from 1% to 10% of methanol in dichloromethane.

Provenance & Evidence