INTERMEDIATE FOR USE IN DOCETAXEL SYNTHESIS AND PRODUCTION METHOD THEREFOR

摘要

1. A chemical compound having the formula 2. A method of producing a compound having the formula comprising the step of acylating 10-deacetyl Baccatin III with at least a 1.5 equivalents of n-butyl lithium and at least 1.5 equivalents of benzyl chloroformate in tetrahydrofuran. 3. A method according to claim 2 wherein the 10-deacetyl Baccatin III is first dissolved in said tetrahydrofuran to form a solution after which said n-butyl lithium is next added to form a first mixture and thereafter said benzyl chloroformate is added to said first mixture to form a second mixture. 4. A method according to claim 3 wherein said n-butyl lithium is in a hexane solution, said n-butyl lithium in hexane being added dropwise to said solution. 5. A method according to claim 3 wherein said solution is cooled to a reduced temperature of -20 degree C. or less prior to adding said n-butyl lithium. 6. A method according to claim 5 wherein the reduced temperature is about -78 degree C. 7. A method according to claim 5 wherein said first mixture is stirred at the reduced temperature for about five minutes and wherein said second mixture is stirred at the reduced temperature for about one hour. 8. A method according to claim 7 wherein said second mixture is quenched with ammonium chloride and thereafter reduced to a residue. 9. A method according to claim 8 including the step of dissolving said residue in organic solvent not misible in water to form a residue solution after which said residue solution is first washed with water and next washed with brine to form an organic layer. 10. A method according to claim 9 including the steps of removing, drying and recrystallizing said organic layer. 11. A method according to claim 10 wherein recrystalization is accomplished with ethyl acetate/hexane. 12. A method according to claim 2 wherein the step of acylating said 10-deacetyl Baccatin III is accomplished with at least two equivalents of n-butyl lithium and at least two equivalents of benzyl chloroformate.