Hydrochloric Acid → 1-Chlorocarbonyl-4-piperidinopiperidine hydrochloride

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Reaction Steps

The present invention is related to a process for the preparation of [1,4′]bipiperidinyl-1′-carbonyl chloride or its hydrochloride, which is a useful intermediate e.g. in the preparation of irinotecan. The use of methylene chloride as a solvent in the reaction of 4-piperidinopiperidine with phosgene and the removal of the reaction solvent by using an additional distillation solvent to raise the distillation temperature gives [1,4′]bipiperidinyl-1′-carbonyl chloride hydrochloride in high yield and purity. The amount of dimer impurity will be less than 5%, even less than 1%.

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