http://rdf.ncbi.nlm.nih.gov/pubchem/patent/YU-46712-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_14effe3850d2129f863b969dac4f1db8 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-35 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-335 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A01N43-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D493-22 |
| filingDate | 1988-08-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_730ca24650e90c4feccc4e1b921934b0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e530b667b64c62c836da2cba0b2b8d6d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_00a6ba577c90c04994f523190241d106 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_08fbc9bea5129f500f8583a0d18e39dc http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cc00dc060d28cf5d56595ac64d4f9ddf http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fb646a239811f8a84fb00c304e7c54ee http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c4fbfcc3e86f712c57cd8cfbe74b4077 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_43756ec85259b4cace956a90aeed97eb http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b22e34cd1306b744b668f662e5e1d6e2 |
| publicationDate | 1994-04-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | YU-46712-B |
| titleOfInvention | PROCEDURE FOR OBTAINING NEW MICROLIDE COMPOUNDS |
| abstract | A process for the preparation of novel MICROLIDE COMPOUNDS of the general formula (I): and salts thereof, wherein in the formula: R1 represents a methyl, ethyl or isopropyl group: R2 represents a hydrogen atom, a C1-4alkyl group or an allyl group and the group = NOR2 is in E -configuration; and OR3 is a hydroxyl group or -OR4 '-OCOR4 or -OCOOR4, wherein R4 is C1-4alkyl or -OCOR8 R9, wherein R8 and R9 are independently hydrogen or C1-4alkyl, wherein to obtain the compound of formula (I) in wherein OR3 is a hydroxyl group, comprising reducing a compound of formula (III) wherein R 1 and R 2 have the above meanings, with a reducing agent selected from the group consisting of alkali metal borohydrides and lithium alkoxyaluminum hydride, preferably with sodium borohydride, in an alkaline such as isopropyl alcohol or isobutyl alcohol, at a temperature in the range of -30 to + 80 ° C, most preferably at 0; then, if necessary, converting the OR3 group to a substituted hydroxyl group by reacting the resulting compound with a reagent selected from the group consisting of an acid of formula R4COOH, or a reactive derivative thereof, such as chloride, anhydride, or activated ester, wherein the reaction is performed in a conventional manner in the presence of a tertiary amine acid scavenger such as diethylamine, pyridine and the like, or a condensing agent such as carbodimide, N, N'-dicyclohexylcarbodimide, the reaction being carried out in non-aqueous media at a temperature in the range - 20 to +100 C; and then, if desired, to form a compound of formula (I) wherein R 2 is a C 1-4 alkyl or C 3 allyl group, a compound of formula (I) wherein R 2 is a hydrogen atom and OR 3 a substituted hydroxyl group, is reacted with an esterifying agent of formula R 2Y, wherein R2 is as defined previously and Y is a leaving group, this reaction being carried out in the usual manner, and finally, if desired, deprotected from the OR3 protected hydroxyl group, and if desired, the compound of formula ( I), in its salts. |
| priorityDate | 1987-04-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 51.