http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2293445-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_8ec818dde59a75c3b5b395e29649c2fa |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D411-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D327-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B61-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D327-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D411-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-04 |
| filingDate | 2002-06-14^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2008-03-16^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_182b8108cf11cc859911e56478d9c4f3 |
| publicationDate | 2008-03-16^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2293445-T3 |
| titleOfInvention | STEREOSSELECTIVE PROCEDURE FOR THE PREPARATION OF NUCLEOSIDE ANALOGS. |
| abstract | A stereoselective process for manufacturing predominantly cis-2-hydroxymethyl-4- (cytosin-1 '' -yl) -1,3-oxathiolane of formula (A1) having cis / trans ratios greater than 2: 1, comprising a first step of coupling a compound of formula (B1): with a base R1, in which R1 is a protected cytosine or a derivative thereof, in a suitable coupling solvent in the presence of a catalytic amount of an element of group IB or IIB selected from Cu +, Cu2 +, Ag +, Au +, Au3 +, Zn2 +, or Cd2 + or combinations thereof; a tertiary amine selected from triethylamine, diethylcyclohexylamine, diethylmethylamine, dimethylethylamine, dimethylisopropylamine, dimethylbutylamine, dimethylcyclohexylamine, tributylamine, or diisopropylethylamine or combinations thereof; and a Lewis acid selected from trimethylsilyltriflate bromotrimethylsilane, iodotrimethylsilane or combinations thereof, to provide an intermediate of formula (D1): wherein R1 is as defined above; and a second step to deprotect the intermediate of formula (D1) to provide the predominantly cis oxathiolanes of formula (A1). |
| priorityDate | 2001-06-15^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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