http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1395641-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2ca2e4410855da087e11bf3eea8933fa |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D263-58 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D263-58 |
| filingDate | 1972-05-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1975-05-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1395641-A |
| titleOfInvention | 2-anilino-benzoxazoles |
| abstract | 1395641 2 - Anilinobenzoxazoles ELI LILLY & CO 3 May 1972 [4 May 1971 18 Oct 1971] 20471/72 Heading C2C Novel 2-anilinobenzoxazoles of the general formula wherein X is a hydrogen atom or a C 1-4 alkyl, phenyl-C 1-3 alkyl, C 1-3 alkoxy, carboxy, carboxy- C 1-3 alkyl, carbanilino, amino-C 1-3 alkyl, mono- or di-C 1-3 alkylamino-C 1-3 alkyl, C 1-3 alkoxy-C 1-3 alkyl, C 1-3 alkylthio, C 1-3 alkylsulphonyl or anilino-C 1-3 alkyl, each of R 1 , R 2 , R 3 and R 4 is a hydrogen, bromine, chlorine or fluorine atom or a trifluoromethyl, C 1-3 alkylthio, C 1-3 alkylsulphonyl, C 1-3 alkyl, carboxy, C 2-4 alkoxycarbonyl, C 1-3 alkoxy, C 1-3 alkoxy-C 1-3 alkyl, phenyl or nitro group, provided that (a) when three of R 1 , R 2 , R 3 and R 4 are hydrogen atoms, the other is a trifluoromethyl, carboxy, carboxy- C 1-3 alkyl, C 1-3 alkoxy-C 1-3 alkyl, C 2-4 alkoxycarbonyl, C 1-3 alkylthio, C 1-3 alkylsulphonyl or phenyl group; (b) when two of R 1 , R 2 , R 3 and R 4 are hydrogen atoms, the others are selected from bromine, chlorine and fluorine atoms and trifluoromethyl, carboxy, C 1-3 alkyl, carboxy- C 1-3 alkyl, C 1-3 alkoxy, C 2-4 alkoxycarbonyl, C 1-3 alkylthio, C 1-3 alkylsulphonyl, phenyl and nitro groups, with the additional limitation that the others are not both phenyl groups or nitro groups; (c) when all of R 1 , R 2 , R 3 and R 4 are hydrogen atoms, X is not a hydrogen atom; and (d) no more than two of R 1 , R 2 , R 3 and R 4 are other than a hydrogen atom, are prepared (i) by reacting 2-chlorobenzoxazole with an aniline of the general formula (ii) when X is other than a hydrogen atom, by reacting the product of (i) wherein X is a hydrogen atom with a halide of the general formula X-halogen (X is other than a hydrogen atom) in the presence of a solution of sodium hydride in a dry solvent; and (iii) when X is a carbanilino group, by reacting the product of (i) wherein X is a hydrogen atom with phenyl isocyanate in tetrahydrofuran. N - n - Butyl - 4 - chloro - 3 - trifluoromethylaniline is prepared by reacting benzoyl chloride with p-chloro-m-trifluoromethyl-aniline, treating the resulting 4<SP>1</SP>-chloro-3<SP>1</SP>-trifluoromethylbenzanilide with sodium hydride and n-butyl bromide and hydrolysing the resulting N-nbutyl - 4<SP>1</SP> - chloro - 3<SP>1</SP> - trifluoromethyl - benzanilide with aqueous-alcoholic NaOH. 2 - (N - Ethoxycarbonylmethyl - 4 - chloro - 3- trifluoromethylanilino)benzoxazole is prepared by reacting 2 - (4 - chloro - 3 - trifluoromethylanilino)benzoxazole with sodium hydride and ethyl bromoacetate. Pharmaceutical and veterinary compositions having immunosuppressant and, in certain cases, antifertility activity comprise, as active ingredient, a 2-anilinobenzoxazole of the first general formula above, in association with a pharmaceutically or veterinarially acceptable carrier therefor. Certain known 2-anilinobenzoxazoles of the first general formula above (without all the provisos) may also be administered to female animals for the purpose of contraception. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6518291-B1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-1366766-A1 |
| priorityDate | 1971-05-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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