http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1476608-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_05a203d85ee01909eaf728dc16f0f6cb |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D265-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D279-02 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D279-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D265-02 |
filingDate | 1975-09-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1977-06-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1476608-A |
titleOfInvention | Preparation of benzothiazine-1,1-dioxide derivatives |
abstract | 1476608 Preparing benzothiazine-1,1-dioxide derivatives PFIZER Inc 23 Sept 1975 [1 Oct 1974] 39034/75 Heading C2C Compounds of the general formula where X and Y are H, F, Cl, Br, CF 3 , NO 2 or C 1-5 alkyl or alkoxy, R 1 is H, C 1-6 alkyl, C 2-4 alkenyl or phenyl-(C 1-3 ) alkyl and R 2 is 2- pyridyl which may be substituted by 3-, 4-, 5- or 6-methyl, 4,6-dimethyl, 3-OH, or 5-Cl, -Br -NO 2 or -CONH 2 ; 2-pyrazinyl, 5-methyl-3- pyrazinyl; 2- or 4-pyrimidyl, 4,5-dimethyl-2- pyrimidyl; 6-methoxy-3-pyridazinyl; 1-phenyl-3-pyrazolonyl; 2-thiazolyl which may be substituted by 4-methyl or -phenyl, 5-Br, or 4,5-dimethyl; 3-isothiazolyl; 2-benzothiazolyl which may be substituted by 4-Cl, or 6-Br or -methyl; 5-Cl-2-benzoxazolyl; 1,3,4-thiadiazolyl, 5-methyl-1,2,4- or -1,3,4-thiadiazolyl; 1,2,4- triazolyl or its 6-phenyl derivative; or 3-isoxazolyl or its 5-methyl derivative, are prepared by reacting with at least an equimolar amount of R 2 NH 2 at 75-200 C. in an inert organic solvent, R 3 being -H, C 1-8 alkyl, phenyl-(C 1-3 ) alkyl, naphthyl, substituted naphthyl or phenyl which may be mono- or di-substituted by F, Cl, Br, NO 2 , CF 3 or C 1-3 alkyl or alkoxy. Many compounds of Formula V (or VI) are prepared in examples and have pharmaceutical properties. Compounds of Formula VII (or VIII) wherein R 3 is H, C 1-4 alkyl, benzyl, phenylethyl, α-(2- chloronaphthyl), #-(1-chloronaphthyl), phenyl or substituted phenyl are prepared by reacting with the appropriate organic isocyanate in the presence of either (C 2 H 5 ) 3 N or NaH. 3,4 - Dihydro - 2 - methyl - 3 - oxo - 2H - 1,2- benzothiazine-1,1-dioxide is prepared by heating 2 - (N - methylsulphamyl) phenyl acetic acid under reflux in the presence of p-toluene sulphonic acid, the substituted acetic acid itself being prepared by reacting N-methyl o-toluene sulphonamide with n-C 4 H 9 Li followed by treatment with ice, H 2 O and HCl. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-2128190-A |
priorityDate | 1974-10-01-04:00^^<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: 34.