http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2014058081-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5f683349ec51134246442157fc2ca82a |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-6561 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F7-1804 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-6561 |
| filingDate | 2013-08-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_49dc997dc9794a6295b1a1784fa37747 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_08c48ec5c84dc054fe3fd191ea7488b5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc233e0a258e8687086824b393e24742 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6d8e5588cbbe51cd5c9f4d062078708e |
| publicationDate | 2014-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-2014058081-A1 |
| titleOfInvention | Method for preparing 42-(dimethylphosphinate) rapamycin |
| abstract | A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) (I) is provided, which has advantages of high conversion rate and no 31,42-bis(dimethyl phosphinate) Rapamycin (III) generated. In the method of the present invention, Rapamycin (II) is firstly reacted with triethyl chlorosilane in a base condition to form 31,42-bis(triethylsilylether) Rapamycin (IV-b), followed by a selective deprotection process to obtain 31-triethylsilylether Rapamycin (V-b). Next, a phosphorylation reaction is performed by using dimethylphosphinic chloride under a base solution to obtain a crude product. Finally, a deprotection reaction is performed in a diluted sulfuric acid solution to obtain a crude product of Ridaforolimus (I). Since the conversion rate of each step of the method of the present invention is higher than 98%, it indicates that the method of the present invention is suitable for industrial production. |
| priorityDate | 2012-08-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 136.