http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IL-122462-A
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_61c0b38c0948cdbce0b193c5279ab4a9 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-41 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-30 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4196 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-505 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-30 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-34 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D249-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D- |
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 |
Incoming Links
Total number of triples: 150.