| Predicate |
Object |
| assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_5305109c4efec4cbcdd8bc05bdb00399 |
| classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-06
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D451-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D451-10 |
| classificationIPCAdditional |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-06
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P11-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-46 |
| classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D451-10
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D451-06 |
| filingDate |
2012-03-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cc3848e2fb717a84dedc2c4a7b783138
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e16b9f012b6f76ebac3fbc3bd86b9f84 |
| publicationDate |
2015-03-25-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber |
CZ-305012-B6 |
| titleOfInvention |
Process for preparing di (2-thienyl) glycolic acid scopine ester intermediate in the synthesis of tiotropium bromide |
| abstract |
The present invention relates to a process for preparing tiotropium bromide of formula II, comprising the steps of:na) preparing a scopine ester of formula I by transesterification of methyl di (2-thienyl) glycolate of formula IV with a scopine of formula III in the presence of a substoichiometric amount of a sterically hindered base selected from the sodium or potassium salt of tert-butoxide, tert-pentoxide, isopropoxide in an inert solvent, wherein the transesterification is carried out at a temperature of 80 to 130 degC and at a pressure in the range of 50 kPa to 30 kPa while the resulting methanol is distilled off;nb) isolating the scopine ester of Formula I;nc) quaternizing the scopine ester of formula I with methyl bromide. |
| priorityDate |
2012-03-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type |
http://data.epo.org/linked-data/def/patent/Publication |