4,10beta-DIACETOXY-2alpha-BENZOYL-OXY-5beta,20-EPOXY-1-HYDROXY-9-OXO-19-NOR-CYCLOPROPA[G]TAX-11-ENE-13alpha-YL (2R,3S)-TERT-BUTOXYCARBONYLAMINO-2-HYDROXY-3-PHENYLPROPIONATE DIHYDRATE, AND METHOD FOR PREPARING SAME

• Main Authors: LAVIGNE, MICHAEL, DIDIER, ERIC, AUTHELIN, JEAN-RENE
• Format: Patent
• Language: English; Russian
• Published: 28.02.2000
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

1. Dihydrate (2R, 3S)-3 tert-butoxycarbonylamino-2-hydroxy-3 phenylpropionate 4,10β-diacetoxy-2α-benzoyl-oxy-5β,20-epoxy-1-hydroxy-9-oxo-19-no-rcyclopropa[g]tax-11-ene-13α-yl. 2. A method for preparing dihydrate (2R, 3S)-3 tert-butoxycarbonylamino-2-hydroxy-3 phenylpropionate 4,10β-diacetoxy-2α-benzoyl-oxy-5β,20-epoxy-1-hydroxy-9-oxo-19-nor-cyclopropa[g]tax-11-ene-13α-yl, charactewrized in that (2R, 3S)-3 tert-butoxycarbonylamino-2-hydroxy-3 phenylpropionate 4,10β-diacetoxy-2α-benzoyl-oxy-5β,20-epoxy-1-hydroxy-9-oxo-19-nor-cyclopropa[g]tax-11-ene-13α-yl or a hydrate thereof is crystallized in a mixture of water and aliphatic alcohol containing from 1 to 3 carbon atomsor in a mixture of water and ketone containing from 3 to 4 carbon atoms, dry the obtained product at a reduced pressure and maintain it, if necessary, under relative humidity above or equal to 40%, or dry the product directly under relative humidity above or equal to 40%. 3. A method as defined in claim 2, characterized in that final volumetric ratio water/alcohol and water/ketone is between 3/1-1/3. 4. A method as defined in claim 2 or 3, characterized in that alcohol is ethanol and ketone is acetone. 5. A method as defined in claim 2, characterized in that drying and possible maintainingare carried out at a temperature of about 40 degree C under pressure of about 5 kPa thus obtaining a stable product having water content of 3-5%. 6. A method as defined in claim 2, characterized in that (2R, 3S)-3 tert-butoxycarbonylamino-2-hydroxy-3 phenylpropionate 4,10β-diacetoxy-2α-benzoyl-oxy-5β, 20-epoxy-1-hydroxy-9-oxo-19-nor-cyclopropa[g]tax-11-ene-13α-yl is used in ethanol solution obtained by deprotection in acid medium from ester (2R, 4S, 5R)-3-tert-butoxycarbonyl-2-(4-methxyphenyl)-4-phenyloxazolidine-5-carboxylate 4,10β-diacetoxy-2α-benzoyl-oxy-5β,20-epoxy-1-hydroxy-9-oxo-19-nor-cyclopropa[g]tax-11-ene-13α-yl.