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publicationDate 2010-12-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber HR-P20100620-T1
titleOfInvention CHEMICAL AND SITUATION SULFONING PROCEDURE
abstract A process for the preparation of a compound of formula IIa: wherein R is a suitable sulfonate ester; from (C1-C6) alkyl-4-piperidinecarboxylate compound according to formula III: which process comprises the following steps: (a) reacting a (C1-C6) alkyl-4-piperidinecarboxylate compound according to formula III with di-tert-butyl dicarbonate in the presence of toluene or xylene forming a first mixture comprising toluene or xylene, tert-butanol and a compound of formula IV: (b) substantially removing tert-butanol from the first mixture; (c) reacting a compound of formula IV with a suitable in situ reducing agent in the presence of toluene or xylene to form a second mixture containing toluene, reducing by-products including alcoholic by-products and a compound of formula V: (d) majority removal of alcoholic by-products -products from another mixture; and (e) reacting a compound of formula V with a suitable in situ sulfonating agent to form a sulfonate ester in the presence of a suitable base and toluene to form a compound of formula IIa. The patent contains 7 more patent claims.
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Total number of triples: 38.