154306-85-1Relevant academic research and scientific papers
Synthesis, cytotoxicity, metabolic stability and pharmacokinetic evaluation of fluorinated docetaxel analogs
Lu, Hong-Fu,Xie, Cheng,Chang, Jun,Lin, Guo-Qiang,Sun, Xun
scheme or table, p. 1743 - 1748 (2011/05/06)
Three novel fluorinated docetaxel analogs, along with six previous reported, were evaluated for their cytotoxicity against five tumor cell lines. The results indicated that these analogs maintained similar/more potent activity than docetaxel against these tumor cell lines. They were also evaluated for their metabolic stability and pharmacokinetics, which demonstrated that these analogs showed better profiles of metabolic stability and pharmacokinetics than that of docetaxel.
Process for the preparation of β-phenylisoserine and β-lactam and their analogues
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, (2008/06/13)
The present invention relates to new process for the preparation of β-phenylisoserine and its analogues of general formula: STR1 which are particularly useful for preparing taxane derivatives which have remarkable antitumour and antileukaemic activities.
Synthesis of taxoids I. Regioselective Lewis acid-mediated ring-opening of aryl orthoacetates
Harada, Naoyuki,Hashiyama, Tomiki,Ozaki, Kunihiko,Yamaguchi, Tetsuo,Ando, Akira,Tsujihara, Kenji
, p. 305 - 318 (2007/10/03)
The reaction of aryl orthoacetates with acetyl bromide readily proceeded regioselectively to afford the desirable aryl bromides in the presence of tin(II) or zinc bromide as a catalyst. The synthesis of some docetaxel derivatives is also described by using this improved process.
Process for the preparation of β-phenylisoserine and its analogues
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, (2008/06/13)
This invention relates to a method for preparing β-phenylisoserine and analogues thereof having general formula (I) STR1 from an aromatic aldehyde and an α-methylarylamine-S, and through a lactam of general formula (II) as described herein. The acids of g
A Practical Access to Chiral Phenylisoserinates, Preparation of Taxotere Analogs
Bourzat, Jean Dominique,Commercon, Alain
, p. 6049 - 6052 (2007/10/02)
A practical diastereoselective synthesis of phenylisoserine methyl esters 8a-c is described using α-methyl-benzylamine as the chiral template of a Staudinger reaction.Optically pure diastereoisomers 6a-c were easily recovered by crystallization.After opening of these intermediate azetidinones by hydrochloric acid and methanol, regioselective cleavage of the chiral auxiliary was achieved by hydrogenation over palladium.Phenylisoserinates 8b,c were used to prepare analogs of Taxotere.
