http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IL-122462-A

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filingDate 1996-07-26-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2001-10-31-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber IL-122462-A
titleOfInvention Preparation of triazoles by organometallic metal attachment to ketones and a number of such new compounds
abstract A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and " Het" is pyrimidinyl optionally substituted by 1 to 3 substitutents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reaction of a compound of the formula: wherein R is as previously defined for a compound of the formula (I), with a compound of the formula: wherein R1 and " Het" are as previously defined for a compound of the formula (I) and X is chloro, bromo or iodo, in the presence of zinc, iodine and/or a Lewis acid and an aprotic organic solvent: said process being optionally followed by conversion of the compound of the formula (I) to an acid addition or base salt thereof. Claimed as novel are the compounds: (i) (2R, 3S) - 3- (4-chloro- 5-fluoropyrimidin-6-yl) -2- (2, 4-difluorophenyl)-1- (1H-1, 2, 4-triazol- 1-yl) butan-2-ol; (ii) an acid addition salt of (2R, 3S/2S, 3R) - or (2R, 3S) - 3- (4-chloro-5- 2622 י" ד בחשון התשס" ב - October 31, 2001 fluoropyrimidin-6-yl) -2-( 2, 4-difluorophenyl) -1- (1H- 1, 2, 4-triazol- 1-yl) butan-2-ol and preferably the hydrochloride salt; (iii) 3-(2, 4-dichloro-5-fluoropyrimidin- 6-yl) -2-(2, 4-difluorophenyl) -1-(1H-1, 2, 4-triazol-1-yl) butan-2-ol, or the (2R, 3S/2S, 3R)- or (2R, 3S)- form thereof, or an acid addition salt of any thereof; (iv) 3-(2-chloro-5-fluoropyrimidin-6-yl) -2-(2, 4-difluorophenyl)-1-(1H-1, 2, 4-triazol-1-yl) butan-2-ol, or the (2R, 3S/2S, 3R) - or (2R, 3S) - form thereof, or an acid addition salt of any thereof; (v) 3-(1-benzyl-5-fluoropyrimidin-6-on- 4yl)-2- (2,4 - difluorophenyl) -1- (1H-1, 2, 4-triazol-1'-yl) butan-2-ol, or the (2R, 3S/2S, 3R) - or (2R, 3S) - form thereof, or an acid addition salt of any thereof; or (vi) 3-(4-chloropyrimidin-6-yl) -2-(2, 4- difluorophenyl) -1-(1H-1, 2,4 - triazol-1-yl) butan-2-ol, or the (2R, 3S/2S, 3R) - or (2R, 3S) - form thereof, or an acid addition salt of any thereof.
priorityDate 1995-08-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 150.