METHOD OF SYNTHESIS OF (2R,3S)-3-TERTIARY-BUTOXYCARBONYLAMINO- -2-HYDROXY-3-PHENYLPROPIONATE-4-ACETOXY-2α-BENZOYLOXY--5β,20- -EPOXY--1,7β,10β-TRIHYDROXY-9-OXO-TAX-11-ENE-13α-YL TRIHYDRATE Russian patent published in 1999 - IPC

Abstract RU 2126397 C1

FIELD: chemical technology, pharmacy. SUBSTANCE: invention relates to a method of synthesis of (2R,3S)-3-tert.-butoxy- -carbonylamino-2-hydroxy-3-phenylpropionate-4-acetoxy--2α- -benzoyloxy-5β,20-epoxy--1,7β,10β-trihydroxy-9-oxo-tax-11-ene--13α- -yl trihydrate that shows antitumor activity. Trihydrate has very low hygroscopicity as compared with other forms of this substance. Method of synthesis involves crystallization of (2R, 3S)-3-tert. -butoxycarbonylamino-2-hydroxy-3-phenyl- -propionate-4-acetoxy--2α-benzoyloxy--5β,, 20-epoxy--1,7β,10β- -trihydroxy-9-oxo-tax-11-ene-13α-yl in a mixture of water and aliphatic alcohol containing 1-3 carbon atoms at weight ratio = 2:1 followed by drying of prepared product, mainly at 40 C, under pressure, mainly at 4-7 kPa, in atmosphere of relative humidity mainly about 80%. Crystallization process is carried out preferably in the presence of ascorbic acid. EFFECT: improved method of synthesis. 5 cl, 2 ex

Similar patents RU2126397C1

Title Year Author Number
ACID ANHYDRIDES, METHOD OF PREPARATION THEREOF, METHODS OF PREPARATION THEREOF, METHODS OF PREPARATION OF TAXOL OR TAXOTERAN 1993
  • Zhan-Manjuel' Ma[Fr]
RU2104274C1
N-BENZYL-β-PHENYLISOSERIN-(2R,3S), METHOD FOR ITS PRODUCTION AND METHOD OF PRODUCTION OF ESTER OF b-PHENYLISOSERIN-(2R,3S) 1991
  • Zhan-P'Er Djushesn[Fr]
  • Mishel' Mjul'Ozer[Fr]
RU2074172C1
4,10-DIACETOXY-2α-BENZOYLOXY-5β,20-EPOXY-1,7β-DIHYDROXY- 9-OXO-TAX-11-ENE-13α-YL-(2R,3S)-3-BENZOYLAMINO-2-HYDROXY-3-PHENYLPROPIONATE TRIHYDRATE AND METHOD OF ITS PREPARING 1996
  • Zhan-Rene Otelehn
  • Ehrik Did'E
  • Frank Levejlle
  • Izabel' Tajep'E
RU2154642C2
METHOD OF PURIFICATION OF 10-DEACETYLBACCATIN-III AND TAXOTER, TAXOTER TRIHYDRATE 1994
  • Andre Djuran
  • Alan Zherbo
  • Rodol'F Margraff
RU2125563C1
METHOD FOR PRODUCTION OF TAXANE DERIVATIVES AND INTERMEDIATES BY THEIR PRODUCTION 1993
  • Alen Kommerson
  • Ehrik Did'E
  • Ehli Fuke
RU2116302C1
METHOD OF SYNTHESIS OF TAXANE DERIVATIVES AND INTERMEDIATE COMPOUNDS OF SYNTHESIS 1993
  • Zhan-Noel' Deni
  • Ehndrju Grin
  • Alis Kanazava
RU2118958C1
DERIVATIVES OF TAXANE 1993
  • Deni Zhan-Noel'
  • Grin Ehndrju
  • Kanazava Alis
RU2188198C2
METHOD FOR PRODUCTION OF DERIVATIVES OF TAXANE 1993
  • Ehli Fuke[Fr]
  • Zhan-Manjuel' Ma[Fr]
RU2103266C1
TAXOIDS, METHODS OF THEIR SYNTHESIS, INTERMEDIATE COMPOUNDS AND PHARMACEUTICAL COMPOSITION 1993
  • Ehrve Bushar
  • Zhan-Dominik Burza
  • Alen Kommerson
RU2139864C1
TAXOID-BASE PHARMACEUTICAL COMPOSITION AND METHOD OF ITS PREPARING 1995
  • Manfred Durr
  • Jorg-Kristian Khager
  • Armin Vendel'
RU2157200C2

RU 2 126 397 C1

Authors

Zhan-Rene Otelen

Zhak Dovez

Ehli Fuk

Bernadet Mandar

Izabel' Tajep'E

Dates

1999-02-20Published

1995-07-07Filed