http://rdf.ncbi.nlm.nih.gov/pubchem/patent/YU-46635-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-547 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D257-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D407-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-41 |
| filingDate | 1989-07-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_902506165880b56354e70a8b4f5c491c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2217c835cb37516c681c3cc2aa8a7044 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_72e1c87578bec4a88647281f6262f51c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_faee8e14b73bb1d0599917a50b4955d2 |
| publicationDate | 1994-01-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | YU-46635-B |
| titleOfInvention | PROCEDURE FOR OBTAINING TETRAZOLE INTERMEDIARIES |
| abstract | A process for the preparation of TETRAZOLE INTERMEDIARS, of the formula: wherein R 1, R 2, R 3, R 4, R 5 and R 6 each independently represent hydrogen, methyl, methoxy or fluoro; and B is C1-6 alkoxycarbonyl, CH2OH or CHO, wherein the benzophenone of formula: wherein R1 'are R2, R3, R4, R5 and R6 as defined above, is reacted with cyanoacetate of formula: CN-CH2-CO2- alk in which alk represents C1-6, in an organic solvent such as benzene or toluene, in the presence of an acid such as acetic acid and catalytic amounts of beta-alanine, at the reflux temperature of the reaction mixture and separating the water formed to give the compound of formula: wherein R 1, R 2, R 3, R 4, R 5 and R 6 and alk are as defined above, after which the resulting compound is reacted with aziodotributylstannane, in the same solvent, at reflux temperature, and the thiazolyl product of formula: sodium in wherein the radicals have the above meanings are treated with sodium hydride, in the same solvent and at a temperature of 40-45 ° C, under an argon atmosphere, and then methylated with methyl iodide to give the product of formula (I) in which B represents C1 -6 alkoxycarbonyl; wherein in the resulting compound, if necessary, the C1-6 alkoxycarbonyl group is converted to the CH2OH group, by saponification with a base such as lithium hydroxide, in a solvent such as tetrahydrofuran and then by hydrolysis with an acid such as hydrochloric acid, by converting the resulting acid into its chloride by reaction with oxalyl chloride in a solvent such as methylene chloride and at room temperature to reflux temperature and finally by reaction of the obtained chloride with lithium aluminum hydride, in a solvent such as tetrahydrofuran and at a temperature of -78 ° C; and thereafter, if necessary, the CH2OH group is converted to the CHO group by reaction with pyridine chlorochromate, at room temperature and in a solvent such as methylene chloride. |
| priorityDate | 1987-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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