http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2014078168-A1

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F7-0812
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filingDate 2013-11-07-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_4dfdd0980f857f9ff6f8bc60717c66e1
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_79a11057c55ddd23ad50fabadb410a3b
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e5dabfe99b17050486fd996c881cc2aa
publicationDate 2014-05-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2014078168-A1
titleOfInvention Methods for the total chemical synthesis of enantiomerically-pure 7-(2'-trimethylsilyl) ethyl camptothecin
abstract The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e. , 99%) 7-(2'-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2'-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7- (trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7- (trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A- ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.
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priorityDate 2012-11-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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