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filingDate 1991-02-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a0d55c55748677831add9dcf453e0a48
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publicationDate 1992-08-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-H04234866-A
titleOfInvention Production of 1,5-benzothiazepine derivative
abstract PURPOSE: To produce a 1,5-benzothiazepine derivative useful as an intermediate for drugs by a process in a high yield by subjecting a propionic acid ester derivative to an intramolecular ring-closing reaction in the presence of a sulfonic acid compound in a specific solvent. n CONSTITUTION: A propionic acid ester of formula I (R 1 is lower alkyl; R 2 is ester residue) is subjected to an intramolecular ring-closing reaction in the presence of a sulfonic acid compound of formula II (R 3 is lower alkyl, phenyl) 10 a non-halogenated organic solvent to produce a 1,5-benzothiazepine derivative of formula III. The compound of formula II is preferably methanesulfonic acid or toluenesulfonic acid. The employment of toluene, ethylbenzene, xylene, n- pentane, etc., as the organic solvent causes the intramolecular ring-closing reaction at 90-160°C, especially 110-145°C. n COPYRIGHT: (C)1992,JPO&Japio
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priorityDate 1990-03-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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