154306-86-2

Upstream product

• 116-11-0 2-Methoxypropene 
• 154306-85-1 methyl (2R,3S)-3-tert-butoxy-carbonylamino-2-hydroxy-3-(4-fluorophenyl)propionate 
• 459-57-4 4-fluorobenzaldehyde 
• 136265-10-6 ethyl 4-fluorocinnamate 
• 459-32-5 (E)-4-fluorocinnamic acid 
• 1300036-08-1 C₁₂H₁₃FO₂ 
• 1300036-09-2 isopropyl (2R,3S)-3-acetylamino-2-hydroxy-3-(4-fluorophenyl)propionate 
• 154306-83-9 (3R,4S)-3-hydroxy-4-(4-fluorophenyl)-1-[(S)-1-phenyl]ethyl-2-azetidinone 
• 154306-84-0 methyl (2R,3S)-2-hydroxy-3-[(S)-1-phenyl]ethylamino-3-(4-fluorophenyl)propionate 
• 157240-38-5 methyl (2R,3S)-3-amino-2-hydroxy-3-(4-fluoro-phenyl)propionate 
• 186758-10-1 (2R,3S)-2-Acetoxy-3-azido-3-(4-fluoro-phenyl)-propionic acid methyl ester 
• 186758-11-2 (2R,3S)-3-Azido-3-(4-fluoro-phenyl)-2-hydroxy-propionic acid methyl ester 
• 186758-13-4 (4R,5S)-5-(4-Fluoro-phenyl)-2-methoxy-2-methyl-[1,3]dioxolane-4-carboxylic acid methyl ester 
• 186758-14-5 (2S,3R)-2-Acetoxy-3-bromo-3-(4-fluoro-phenyl)-propionic acid methyl ester 

Downstream Products

• 143527-61-1 3'-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 143527-60-0 C₄₉H₅₄Cl₆FNO₁₈ 
• 143527-63-3 C₅₂H₅₈Cl₆FNO₁₈ 
• 1300036-11-6 N-de-tert-butoxycarbonyl-N-[2-(1-fluoro-2-methyl)propyloxycarbonyl]-7,10-di-(2,2,2-trichloroethyloxycarbonyl)-3-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 1300036-12-7 N-de-tert-butoxycarbonyl-N-[2-(1,1-difluoro-2-methyl)propyloxycarbonyl]-7,10-di-(2,2,2-trichloroethyloxycarbonyl)-3-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 1300036-13-8 N-de-tert-butoxycarbonyl-N-[2-(1,1,1-trifluoro-2-methyl)propyloxycarbonyl]-7,10-di-(2,2,2-trichloroethyloxycarbonyl)-3-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 1300036-07-0 N-de-tert-butoxycarbonyl-N-[2-(1-fluoro-2-methyl)propyloxycarbonyl]-3-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 1300036-14-9 N-de-tert-butoxycarbonyl-N-[2-(1,1-difluoro-2-methyl)propyloxycarbonyl]-3-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 1300036-15-0 N-de-tert-butoxycarbonyl-N-[2-(1,1,1-trifluoro-2-methyl)propyloxycarbonyl]-3-dephenyl-3'-(4-fluorophenyl)docetaxel 
• 143527-64-4 (4S,5R)-4-(4-Fluoro-phenyl)-2,2-dimethyl-oxazolidine-3,5-dicarboxylic acid 3-tert-butyl ester 

Relevant academic research and scientific papers

Synthesis, cytotoxicity, metabolic stability and pharmacokinetic evaluation of fluorinated docetaxel analogs

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.

Synthesis of taxoids I. Regioselective Lewis acid-mediated ring-opening of aryl orthoacetates

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.

A Practical Access to Chiral Phenylisoserinates, Preparation of Taxotere Analogs

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.