- Improved protection and esterification of a precursor of the taxotere and taxol side chains
-
(4S,5R)-N-BOC-2,2-dimethyl-4-phenyl-5-oxazolidinecarboxylic acid 8 was prepared and efficiently esterified by conveniently protected baccatins 9a,b. Smooth deprotection in formic acid gave the N-deprotected intermediates of Taxotere and taxol. This protocol did not generate any epimerization at C-2′ and constitutes a pratical method to prepare Taxotere, taxol and analogs.
- Commercon,Bezard,Bernard,Bourzat
-
-
Read Online
- Semisynthesis method for docetaxel
-
The invention relates to a semisynthesis method for docetaxel. The semisynthesis method comprises the following steps: protecting hydroxyl groups on 7-carbon and 10-carbon on 10-DAB III by using chloroformic acid-2,2,2-trichloroethyl ester so as to obtain an intermediate I, performing a condensation reaction on the intermediate I and a five-membered ring side chain so as to obtain an intermediateII, performing ring opening on the intermediate II under the action of hydrochloric acid to remove a protecting group on the five-membered ring side chain so as to obtain an intermediate III, and removing a Troc protecting group from the intermediate III under an acidic condition so as to obtain the docetaxel. The semisynthesis method provided by the invention has the advantages of simple processroute, mild reaction conditions, fewer impurities generated in the reaction process, higher yield and stable properties of obtained intermediates, and applicability to industrial large-scale production.
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- Synthesis of Taxol and Docetaxel by Using 10-Deacetyl-7-xylosyltaxanes
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A mixture of taxols was prepared from 10-deacetyl-7-xylosyltaxanes by three-step reactions: redox, acetylation, and deacetylation. The mixture was separated by column chromatography on silica gel to afford Taxol, Taxol B (Cephalomannine) and Taxol C. The mixture of Taxol B and Taxol C was converted to Docetaxel by Schwartz's reagent. The structures of Taxol and Docetaxel were characterized by HPLC, 1H-NMR, 13C-NMR and MS. This synthetic process has expanded the source of biomass for the chemical semi-synthesis of Taxol and Docetaxel, reduced the production costs, and increased the biomass resource of taxanes.
- Xue, Baoyu,Zhao, Junhong,Fan, Yange,Chen, Shipeng,Li, Wenfeng,Chen, Jin,Li, Zheng,Wang, Hongxing,Kong, Hongjun
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-
- Method for synthesizing cabazitaxel from 10-deacetylbaccatin III
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The invention discloses a method for synthesizing cabazitaxel from 10-deacetylbaccatin III. According to the method, 10-deacetylbaccatin III is used as a raw material, and 7,10-(di)Troc-10-DAB is prepared in the presence of a solvent, a catalyst and chloroformic acid 2, 2, 2-trichloroethyl ester; then 7,10-(di)Troc-10-DAB is condensed with a side chain of docetaxel to prepare an intermediate II, the intermediate II is subjected to protective group removal to obtain a kappa precursor I, the kappa precursor I is further prepared into a kappa precursor II, the kappa precursor II is subjected to sulfur methyl removal, and then is hydrolyzed under acidic conditions to obtain crude cabazitaxel; the crude cabazitaxel is subjected to recrystallization, column chromatography, recrystallization andpurification to obtain the cabazitaxel with the content being greater than 99%. The method provided by the invention has the advantages that the reaction conditions are mild and controllable, some ofthe reactions can be carried out in one pot, a methylation reagent used is a non-toxic reagent, and is safe, reliable, low in cost and high in yield, and the obtained product is high in purity, less in impurity content, and suitable for industrial production and marketing applications.
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- Formulation optimization of an ephrin A2 targeted immunoliposome encapsulating reversibly modified taxane prodrugs
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Ephrin A2 targeted immunoliposomes incorporating pH-sensitive taxane prodrugs were developed for sustained delivery of active drug to solid tumors. Here we describe the systematic formulation development and characterization of these immunoliposomes. We s
- Huang, Zhaohua Richard,Tipparaju, Suresh Kumar,Kirpotin, Dmitri B.,Pien, Christine,Kornaga, Tad,Noble, Charles O.,Koshkaryev, Alexander,Tran, Jimmy,Kamoun, Walid S.,Drummond, Daryl C.
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- Method for purifying docetaxel
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The invention discloses a method for purifying docetaxel. A docetaxel solid precipitates from a dichloromethane and toluene mixed solution. The purifying method has the advantages of great reduction of the single content of every impurity in docetaxel, introduction of few impurities, improvement of the purity of the product, and high yield, and is very suitable for industrial large-scale production, and the obtained product meets preparation demands, and can be directly used to prepare a docetaxel injection.
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- Synthesis method of docetaxel
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The invention provides a synthesis technology of docetaxel. The synthesis technology comprises the following steps: with double-protection 10-DAB of a structure shown as a formula I as a raw material,performing condensation reaction between the double-pro
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Paragraph 0040-0042; 0047-0049; 0054-0056; 0061-0063
(2018/03/24)
-
- Method for semisynthesis of Docetaxel and intermediate of Docetaxel
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The invention relates to a method for semisynthesis of Docetaxel and an intermediate of the Docetaxel. The method provided by the invention comprises the steps of firstly, carrying out hydroxyl protection on C7 and C10 of 10-DAB III (10-deacetylbaccatin III) by using 2,2,2-trichloroethylchloroformate so as to obtain an intermediate I, subjecting the intermediate I to a reaction with a side chain radical compound so as to prepare an intermediate II, subjecting the intermediate II to a hydrogenation reaction under the catalysis of palladium-charcoal so as to prepare an intermediate III, subjecting the intermediate III to a reaction under acidic conditions so as to obtain a Docetaxel crude product, and subjecting the Docetaxel crude product to purification, thereby obtaining a purified product. According to the method provided by the invention, the 10-DAB III raw material can be sufficiently utilized, finally-produced byproducts are few, the final product Docetaxel has the purity of 99.6% to 99.9%, the mole yield reaches up to 73% to 82%, and the utilization ratio of the 10-DAB III can be greatly increased.
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Paragraph 0051-0055; 0065-0069; 0079-0083
(2017/10/27)
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- EPHRIN RECEPTOR A2 (EPHA2)-TARGETED DOCETAXEL-GENERATING NANO-LIPOSOME COMPOSITIONS
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EphA2-targeted immunoliposomes for delivering docetaxel are useful in the treatment of certain types of cancer. The immunoliposomes can include an EphA2 targeting moiety (e.g., a scFv) and encapsulate a docetaxel prodrug in a stable salt form within a liposome having an average size of about 100 nm. Novel docetaxel prodrugs suitable for loading into nanoliposomes (including immunoliposomes) are provided, along with novel and other useful EphA2 targeting moieties for preparation of EphA2-targeted doxorubicin-generating immunoliposome therapies. Pharmaceutical compositions can be prepared that include nanoliposomes encapsulating one or more docetaxel prodrugs, and/or immunoliposomes or nanoparticles comprising an EphA2 binding moiety and encapsulating one or more docetaxel prodrugs. The pharmaceutical compositions are useful for administration to a patient for the treatment of cancer.
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Page/Page column 60-61
(2017/10/11)
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- NEW EFFICIENT METHODS FOR THE SYNTHESIS OF TAXANE DERIVATIVES SUCH AS DOCETAXEL AND THEIR STRUCTURAL ANALOGOUS, AND A METHOD FOR THE PREPARATION THEREOF
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The present invention relates to a novel process for the preparation of taxanes such as Docetaxel, a very important anticancer drug. Docetaxel 1 is a clinically well-established anti -mitotic chemotherapy medication used mainly for the treatment of breast
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- Biological evaluation of new antitumor taxoids: Alteration of substitution at the C-7 and C-10 of docetaxel
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A series of new docetaxol analogues have been designed and synthesized. And their cytotoxicities against cancer cells have been evaluated by MTT method. Most of these compounds showed selective inhibitions on human cancer cell lines. Among them, compound 8 exhibited higher inhibitory activity than Paclitaxel (Taxol) against several cancer cell lines. This work indicated that appropriate modification at C-7 and C-10 of docetaxel might be a promising approach for this unique class of anticancer compounds.
- Li, Caihong,Qiu, Yatao,Li, Xing,Liu, Nianjin,Yao, Zhiyi
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supporting information
p. 855 - 859
(2014/02/14)
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- Particle replication in nonwetting templates nanoparticles with tumor selective alkyl silyl ether docetaxel prodrug reduces toxicity
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Delivery systems designed to have triggered release after passively targeting the tumor may improve small molecule chemotherapeutic delivery. Particle replication in nonwetting templates was used to prepare nanoparticles to passively target solid tumors i
- Chu, Kevin S.,Finniss, Mathew C.,Schorzman, Allison N.,Kuijer, Jennifer L.,Luft, J. Christopher,Bowerman, Charles J.,Napier, Mary E.,Haroon, Zishan A.,Zamboni, William C.,DeSimone, Joseph M.
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p. 1472 - 1476
(2014/04/03)
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- An efficient semi-synthetic method to construct docetaxel via sterically crowded linear side chain esterification
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An efficient semi-synthetic method was developed to construct docetaxel 1 by using N,N-di-Boc protected linear isoserine derivative 5 as the side chain source, in which, bulky protecting group on the nitrogen atom blocked C-2′ position and prohibited unav
- Shen, Xin,Yang, Jidong,Zhan, Huaxing,Wang, Hu,Wu, Shaohong,Chen, Zili
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- Alternative synthesis and the determination of absolute configuration of docetaxel, an anticancer drug
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A simple, efficient, and alternative synthetic route for docetaxel with better control on the protection-deprotection sequence has been developed. The process is easily scalable and commercially viable, and critical impurities can be controlled efficiently. For the first time, absolute configuration of docetaxel was determined unambiguously by single-crystal X-ray diffraction.
- Sekhar,Vishweshwar, Peddy,Acharyulu, Palle V. R.,Anjaneyulu, Yerramilli
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experimental part
p. 3482 - 3492
(2012/10/18)
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- PROCESS FOR PREPARING DOCETAXEL AND ITS HYDRATE
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Disclosed is a process of preparation of (2R,3S)-N-carboxy-3-phenylisoserine, N-tert-butyl ester, 13-ester with 5(P)-20-epoxy-l,2(a), 4,7(P), 10(β), 13(a)-hexa hydroxyl tax-l l-en-9-one 4-acetate 2-benzoate (docetaxel) and its trihydrate (I).
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Page/Page column 17; 21-22
(2012/10/18)
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- PROCESS FOR PREPARING TAXOIDS FROM BACCATIN DERIVATIVES USING LEWIS ACID CATALYST
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The present invention relates to a process of preparing a taxoid (X) by reacting a protected baccatin derivative (B) with a β-lactam (C) in the presence of one or more Lewis acids and a base agent. The present invention also relates to a process of preparing the protected baccatin derivative (B) from a baccatin derivative (A) comprising a protection reaction catalyzed by one or more Lewis acids with an optional base agent.
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- METHOD FOR PREPARING TAXANE DERIVATIVES
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Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a reversion of the stereochemical structure of a selectively separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.
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- One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel
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A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction of protecting the C-7 and C-10 positions a
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Page/Page column 20
(2012/11/06)
-
- NOVEL AMINO ACID MOLECULE AND USES THEREOF
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There is provided novel amino acid molecules and processes for their preparation. There is also provided novel amino acid molecules and their use in processes for preparing the compounds that are useful for the synthesis of paclitaxel, and docetaxel, the anticancer drug.
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Page/Page column 25; 34; 37
(2011/11/12)
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- NOVEL HYDRAZIDE CONTAINING TAXANE CONJUGATES
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The present invention relates to compounds of formula I or salts thereof, wherein, R1 is selected from the group consisting of hydrogen and R4; R2 is selected from the group consisting of hydrogen, acetyl and R4
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Page/Page column 13
(2011/08/02)
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- METHOD FOR PREPARING HIGHLY PURE ANHYDROUS CRYSTALLINE DOCETAXEL
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A method for preparing highly pure anhydrous crystalline docetaxel is provided. The method for preparing highly pure anhydrous crystalline docetaxel enables preparation of anhydrous crystalline docetaxel that has purity of 99.5% or more, and is useful as
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Page/Page column 19-23
(2011/07/30)
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- A Mild and Convenient Semi-Synthesis of Docetaxel from 10-Deacetyl Baccatin III
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A novel protocol for the semi-synthesis of docetaxel was achieved in four steps from 10-deacetyl baccatin III with an overall yield of 50%. The key step is the selective protection of the C(7) and C(10) hydroxyl groups of 10-deacetyl baccatin III, utilizi
- Zhou, Hui,Chen, Dahai,Gao, Hongwei,Li, Qingeng
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p. 450 - 452
(2011/09/14)
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- METHOD FOR PREPARING TAXANE DERIVATIVES
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Provided is a method for preparing a taxane derivative, comprising: carrying out condensation of a phenylisoserine derivatives having a protective group introduced thereto or a mixture of isomers thereof, as a side chain, with a baccatin III derivative or 10-deacetyl-baccatin III derivative to obtain a mixture of isomers; separating the isomers via chromatography; and carrying out a selective reversion of the stereochemical structure of a separated isomer, which is suitable for producing a taxane derivative in a large scale with high yield.
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Page/Page column 18-19
(2010/11/05)
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- PREPARATION OF β-PHENYL-ISOSERINE DERIVATIVES
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A process for stereoselective synthesis of a β-phenylisoserine comprises reacting a carbonyl imine R-C=N-CO-OR1 with a protected α- oxyaldehyde X1O-CH2CHO in the presence of a chiral amine catalyst and oxidizing aldehyde s
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Page/Page column 22-23
(2010/04/06)
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- METHOD OF PREPARING TAXANE DERIVATIVES AND INTERMEDIATES USED THEREIN
-
The present invention relates to a novel method of preparing a taxane derivative having an anti-tumor and anti-leukemia activity, and intermediates used therein.
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Page/Page column 6
(2010/12/29)
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- PROCESS FOR THE PREPARATION OF DOCETAXEL, ITS INTERMEDIATES, AND METHODS FOR PREPARATION THEREOF
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The present invention disclosed an process for preparing docetaxel 1, including the following steps: a) hydroxyl acylation reaction of compound 2 and 3 to obtain compound 4; b) deprotection group R1 of the hydroxyl group of compound 4 obtained
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Page/Page column 8
(2010/12/29)
-
- PREPARATION OF DOCETAXEL
-
The present invention relates to docetaxel and processes for preparing docetaxel, including process-related intermediates. The present invention also relates to processes for preparing substantially pure docetaxel and intermediates.
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Page/Page column 25
(2010/07/10)
-
- SOLVATES OF 4-ACETOXY-2α-BENZOYLOXY-5β,20-EPOXY-1,7β,10β-TRIHYDROXY-9-OXO-TAX-11 -EN- 13α-YL (2R,3S)-3-TERT-BUTOXYCARBONYLAMINO-2-HYDROXY-3-PHENYLPROPIONATE
-
The present invention provides solvates of 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1,7β,10β- trihydroxy-9-oxo-tax-11 -en-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3- phenylpropionate and C2-3-alkyl esters of formic acid, process of their preparation
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Page/Page column 24
(2010/12/26)
-
- PROCESS FOR CONVERTING 9-DIHYDRO-13-ACETYLBACCATIN III INTO DOCETAXEL OR PACLITAXEL
-
Processes for the preparation of docetaxel and paclitaxel or analogs from 9-dihydro-13-acetylbaccatin III via key intermediates (4), (5), (6), (6'), (8) and (8') or via intermediate (12) as well as processes for the preparation of said intermediates are d
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Page/Page column 50; 53
(2009/04/25)
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- A NOVEL PROCESS FOR THE PREPARATION OF DOCETAXEL
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A novel process is outlined for the synthesis or preparation of docetaxel with the help of novel alloy for the deprotection of the protected docetaxel and its conversion into docetaxel.
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Page/Page column 4-7
(2009/05/29)
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- DOCETAXEL PROCESS AND POLYMORPHS
-
Processes for preparing substantially pure docetaxel, new crystalline forms of docetaxel and processes for preparation thereof, processes for preparing docetaxel trihydrate, and pharmaceutical compositions comprising docetaxel.
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Page/Page column 33
(2009/03/07)
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- Method for Preparing Docetaxel
-
The invention concerns a method for preparing docetaxel from paclitaxel, including the following steps: a) deacylating paclitaxel, b) protecting the free hydroxy functions, in 7-, 10- and 2′-position respectively, c) debenzoylating the amine in 3′-position, into a primary amine derived for 10-deacetylbaccatine whereof the hydroxy functions in 7-, 10- and 2′-position are protected, d) functionalizing the amine with a t-butoxycarbonyl In radical to obtain a docetaxel derivative of general formula (I), wherein: X represents protecting radicals or hydrogen atoms, then, if required, e) releasing the initially protected hydroxy functions to obtain docetaxel.
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Page/Page column 3
(2008/12/08)
-
- Crystalline forms of docetaxel and process for preparation thereof
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New anhydrous crystalline form of docetaxel and process of making anhydrous docetaxel and docetaxel trihydrate are provided.
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Page/Page column 3
(2008/12/04)
-
- DOCETAXEL / MONO PROPYLENE GLYCOL CLATHRATE AND METHOD FOR THE PREPARATION THEREOF
-
The present invention relates to a docetaxel / mono propylene glycol clathrate of formula (I) and a method for preparing same. The inventive docetaxel / mono propylene glycol clathrate having a low 7-epimer content and high stability can be advantageously used as an ingredient for the development of a therapeutic agent having anti-tumor and anti-leukemia activities.
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Page/Page column 10-11
(2008/12/04)
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- METHOD OF PREPARING TAXANE DERIVATIVES AND INTERMEDIATES USED THEREIN
-
The present invention relates to a novel method of preparing a taxane derivative having an anti-tumor and anti-leukemia activity, and intermediates used therein.
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Page/Page column 15
(2008/12/06)
-
- METHOD OF PREPARING DOCETAXEL AND INTERMEDIATES USED THEREIN
-
The present invention relates to a novel method for preparing docetaxel having anti-tumor and anti-leukemia activity, and intermediates used therein.
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Page/Page column 17-18; 20-21
(2008/12/06)
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- AMORPHOUS FORM OF DOCETAXEL
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A process for preparation of Amorphous Form of Docetaxel comprising: i. preparation of a solution or suspension of Docetaxel in an organic solvent or mixtures thereof; ii. evaporation of the solvent or mixtures thereof from the solution or suspension of s
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Page/Page column 11
(2008/12/08)
-
- ONE POT SYNTHESIS OF TAXANE DERIVATIVES AND THEIR CONVERSION TO PACLITAXEL AND DOCETAXEL
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A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction, of protecting the C-10 and attaching a si
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Page/Page column 33
(2010/11/30)
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- SEMI-SYNTHETIC ROUTE FOR THE PREPARATION OF PACLITAXEL, DOCETAXEL, AND 10-DEACETYLBACCATIN III FROM 9-DIHYDRO-13-ACETYLBACCATIN III
-
A novel semisynthetic route has been provided in the preparation of docetaxel and paclitaxel. This new process involves the conversion of 9-dihydro-13-acetylbaccatinIII to docetaxel and paclitaxel by the step of converting 9-dihydro-13-acetylbaccatin III into 7-O-triethylsilyl-9,10-diketobaccatin III, and adding docetaxel and paclitaxel side chain precursors, respectively, to form a new class of taxane intermediates, such as 7-O-triethylsilyl-9,10-diketodocetaxel and 7-O-triethylsilyl-9,10-diketopaclitaxeltaxel. These new intermediates then by a series reduction, acetylation of the 10-hydroxyl position for paclitaxel and finally deprotection to yield docetaxel and paclitaxel, the most important anti-cancer drugs.
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Page/Page column 8
(2008/06/13)
-
- NOVEL COMPOUNDS AND METHODS FOR FORMING TAXANES AND USING THE SAME
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The present invention is broadly directed to novel compounds useful for the synthesis of biologically active compounds. More particularly, the present embodiments disclosed herein relate to novel side chains, that when coupled to a taxane, are useful for the synthesis of pharmaceutically useful taxanes. Methods of forming the novel side chains and coupling them to hindered alcohols, namely taxanes resulting in useful esters are also disclosed. Various taxanes compounds are known to exhibit anti-tumor activity.
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Page/Page column 25
(2008/06/13)
-
- DOCETAXEL POLYMORPHS AND PROCESSES
-
The present invention provides crystalline polymorphs of docetaxel and processes for preparing them, a method for preparing amorphous docetaxel, and a process for preparing docetaxel.
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Page/Page column title page; 30-31; 1/31
(2008/06/13)
-
- Crystalline forms of docetaxel and processes for their preparation
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Novel forms of crystalline docetaxel are provided, as well as pharmaceutical compositions, and methods of treatment. Novel processes for making crystalline docetaxel are also provided.
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Page/Page column 6
(2008/06/13)
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- Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid
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The synthesis of docetaxel esters of malic acid is described. These compounds were found to have greatly improved water solubility and are stable in solution at neutral pH. The C2′ modified compounds 2a-c and 3a-c behave as prodrugs, that is, docetaxel is
- Du, Wenting,Hong, Lan,Yao, Tongwei,Yang, Xiaochun,He, Qiaojun,Yang, Bo,Hu, Yongzhou
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p. 6323 - 6330
(2008/04/12)
-
- SEMISYNTHESIS PROCESS FOR THE PREPARATION OF 10-DEACETYL-N-DEBENZOYL-PACLITAXEL
-
The invention relates to a process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel, a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. The invention also discloses a process f
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Page/Page column 13; 14
(2008/06/13)
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- PROCESS FOR THE PREPARATION OF ANHYDROUS AND HYDRATED ACTIVE PHARMACEUTICAL INGREDIENTS (APIS); STABLE PHARMACEUTICAL COMPOSITIONS PREPARED FROM THE SAME AND USES OF SAID COMPOSITIONS
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This invention describes a process for the production of ANHYDROUS active pharmaceutical ingredients (APIs); a process for the preparation of HYDRATED active pharmaceutical ingredients, a process for the preparation of sterile and stable injectable soluti
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Page/Page column 23
(2008/06/13)
-
- Semi-synthetic conversion of paclitaxel to docetaxel
-
A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2′, C-7 and C-10 and introducing a t-Boc
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Page/Page column 14
(2008/06/13)
-
- A novel method to synthesize docetaxel and its isomer with high yields
-
Side chains of docetaxel and its isomer were obtained through Staudinger cycloaddition and catalytic hydrogenation of chlorophenyl intermediates, using chlorobenzaldehyde as starting material. Syntheses of three novel chiral azetidinone derivatives through the Staudinger cycloaddition reaction of chlorophenyl chiral amine Schiff base with different substituted positions were described and their ring-opening reaction under the catalysis of Pd/MgCO 3 or Pd/C to afford side chains of docetaxel and its isomer in high yields was investigated. Finally, docetaxel and its isomer were obtained. Single crystal of (3S,4R)-3-hydroxy-N-[(S)(1-phenyl)ethyl]-4 -(2′-chlorophenyl) -2-azetidinone (4c) was obtained, the configuration of which was determined by X-ray diffraction. Because of the mild cyclization reaction condition and convenient asymmetric resolution operation when p-chlorobenzaldehyde was employed instead of benzaldehyde, the yield of cyclization and hydrogenation increased dramatically and the total yield of docetaxel was higher than the result in literature. When o-chlorobenzaldehyde was employed instead of benzaldehyde an isomer of docetaxel was obtained by the same way.
- Qi, Chuan-Min,Wang, Yun-Feng,Yang, Ling-Chun
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p. 679 - 684
(2007/10/03)
-
- One pot synthesis of taxane derivatives and their conversion to paclitaxel and docetaxel
-
A process is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel, in particular, the semi-synthesis of protected taxane intermediate in a one pot reaction of protecting the C-7, 10 and attaching a
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Page/Page column 11
(2010/02/15)
-
- Semi-synthesis of taxane intermediates and aziridine analogues and their conversion to paclitaxel and docetaxel
-
A process is provided for the semi-synthesis of taxane intermediates and aziridine analogues of cephalomannne and baccatin III intermediates, and the conversion of such intermediates and analogues to paclitaxel and docetaxel.
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Page/Page column 9
(2008/06/13)
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- Radiosynthesis of [11C]docetaxel
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Docetaxel (Taxotere) is an accepted chemotherapeutic agent for the treatment of breast cancer and non-small cell lung cancers. A potential means of predicting response is measuring tumor uptake of [11C]docetaxel using Positron Emission Tomograp
- Van Tilburg,Franssen,Van Der Hoeven,Van Der Meij,Elshove,Lammertsma,Windhorst
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p. 763 - 777
(2007/10/03)
-
- Anticancer taxanes such as paclitaxel, docetaxel and their structural analogs, and a method for the preparation thereof
-
A process for the preparation of taxanes comprising wherein R is a tert. butoxycarbonyl or benzoyl group; PMP is p-methoxyphenyl group; G1 is acetyl group; G2 is haloacetyl group comprising a) protecting the C-7 hydroxyl group of 10-
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