FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes 7-deoxyderivatives of taxol of the formula (I) where R1 means a group of the formula -C(O)Rz where Rz is a group of the formula RO or R and R means C1-C6--alkyl, phenyl; Rg is phenyl or 5-membered heteroaryl containing one atom of oxygen or sulfur; R2 means hydrogen atom or a group of the formula: -COOR where R means C1-C6-alkyl. Also, invention relates to derivatives of baccatine-III (II) that are intermediate compounds in synthesis of 7-deoxyderivatives of taxol of the formula (I) and particular intermediate compounds: 10-penta-fluorothioncarbonate-7-triethylsilylhydroxybaccatine-III of the formula (III), 7-[(methylthio)carbonothioylhydroxy]-10- -deacetylhydroxybaccatine-III of the formula (IV) and 7-[(methylthio)carbonothioylhydroxy] -13-triethylsilhydroxy-baccatine-III of the formula (V) using for synthesis of derivatives of baccatine-III of the formula (II). Also, invention proposes a pharmaceutical composition containing a compound of the formula (I) that shows antitumor activity and can be used for treatment of mammals with tumors. EFFECT: improved method of synthesis, enhanced effectiveness. 14 cl, 1 tbl, 42 ex
Title |
Year |
Author |
Number |
FLUOROTAXOLS, INTERMEDIATE COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHOD OF PATIENT TREATMENT |
1993 |
- Shu-Kh'Ju Chen
- Vittorio Farina
- Dolatraj Vias
- Dzhojdip Kant
|
RU2131874C1 |
6,7-MODIFIED PACLITAXELS AND INTERMEDIATE COMPOUNDS |
1993 |
- Shu-Kh'Ju Chen
- Vittorio Farina
- Gregori Rot
- Dzhon Kehdou
|
RU2125998C1 |
TAXANE DERIVATIVE PHOSPHONOOXYMETHYL ESTERS, INTERMEDIATE COMPOUNDS, ANTITUMOR PHARMACEUTICAL COMPOSITION, METHOD OF TUMOR GROWTH SUPPRESSION IN MAMMALS |
1993 |
- Erzhi Golik
- Dolatraj Vias
- Dzhon Dzh. Rajt
- Genri Vong
- Dzhon F.Kadou
- Dzhon K.Totatil
- Ven-Sen Li
- Murrej A.Kaplan
- Robert K.Perron
|
RU2136673C1 |
PACLITAXEL DERIVATIVES, PHARMACEUTICAL COMPOSITION AND METHOD OF TUMOR GROWTH INHIBITION |
1996 |
- Pol M. Skola
- Dzhon F. Kehdou
- Dolatraj M. Vias
|
RU2162082C2 |
SIDE CHAIN TAXANES, INTERMEDIATE COMPOUNDS, AND METHODS OR PREPARING, THEREOF |
1993 |
- Mikaehl A.Poss
- Dehvid Dzh.Kusera
- Dzherom L.Moniot
- Dzhon K.Tottatil
- Ivan D.Trifunovich
- Shu-Kh'Ju Chen
- Dzhanmej Vej
|
RU2125042C1 |
CIS-N-IMINOMETHYL-3,4-DISUBSTITUTED-β-LACTAMS AND METHODS OF PREPARING CIS-3,4-DISUBSTITUTED-β-LACTAMS, AND USE THEREOF |
1994 |
- Allan V.Rehj
- Parashotam Vemishetti
- Roberto Drogini
|
RU2132844C1 |
DERIVATIVES OF N-ACYL-2-ARYLCYCLOALKYLAMINE STIMULATING MELATONIN SYNTHESIS, PHARMACEUTICAL COMPOSITION, METHOD OF MELATONIN-STIMULATING BINDING |
1996 |
- Dehniel Dzh. Kivi
- Majkl F. Parker
- Ronal'D Dzh. Mehttson
- Grehkham Dzhonson
|
RU2162076C2 |
3-SUBSTITUTED OXINDOLE DERIVATIVES AS MODULATORS OF POTASSIUM CHANNELS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT |
1996 |
- Pijasena Khevavasam
- Nikolas A. Minvell
- Valentin K. Gribkov
|
RU2165925C2 |
BIPHENYLISOXAZOLSULFONAMIDES |
1995 |
- Nejtsen M'Jurudzhsan
- Dzhoel S. Berrish
|
RU2174979C2 |
RETINOID-LIKE COMPOUNDS, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT |
1996 |
- Dzhon E. Stehrrehtt Ml.
- Kuo-Long Ju.
- Muzammil M. Mansuri
- Dehvid R. Tortolani
- Peter R. Rezhek
|
RU2163590C2 |