632335-31-0

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 632335-27-4 7,10-di-O-[2-(chloroacetyl)]-13-[(4S,5R)-2-p-methoxyphenyl-4-phenyl-3-[(2-phenyl-2-trimethylsilyl)ethoxycarbonyl]-1,3-oxazolidinyl-5carbonyl]-10-deacetylbaccatin III 
• 196404-55-4 acide (4S,5R)-N-(tert-butoxycarbonyl)-2-(4-O-methoxyphenyl)-4-phenyl-5-oxazolidine carboxylique 
• 1401086-20-1 7,10-di-O-chloroacetyl-2'-O-benzyl docetaxel 
• 500726-10-3 7,10-di-O-chloroacetyl-10-deacetylbaccatin III 
• 32981-86-5 10-deacetylbaccatin III 

Downstream Products

• 114915-20-7 Docetaxel 

Relevant academic research and scientific papers

NEW EFFICIENT METHODS FOR THE SYNTHESIS OF TAXANE DERIVATIVES SUCH AS DOCETAXEL AND THEIR STRUCTURAL ANALOGOUS, AND A METHOD FOR THE PREPARATION THEREOF

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

PROCESS FOR PREPARING DOCETAXEL AND ITS HYDRATE

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).

Method of preparation of anticancer taxanes using 3-[(substituted-2-trialkylsilyl)ethoxycarbonyl]-5-oxazolidine carboxylic acids

This invention relates to a process for preparation of taxanes comprising subjecting 7,10-diprotected intermediates 7-O-(2-haloacyl) baccatin III 6c or 7,10-O-di-(2-haloacyl)-10-deacetylbaccatin III 6b to a step of coupling with (4S,5R)-3-[(2-alkyl/aryl-2-trialkylsilyl) ethoxy-carbonyl]-4-aryl-2-substituted-1,3-oxazolidine-5-carboxylic acid 1 in the presence of a condensation agent, an activating agent and an aromatic hydrocarbon to obtain 7-O-[2-(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3(2-unsubstituted/substituted-2-trialkylsilyl)-ethoxycarbonyl-1,3-oxazolidinyl-5-carbonyl]baccatin III 7a or 7,10-di-O[2-(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3-(2-unsubstituted/substituted-2-trialkylsilyl)ethoxy-carbonyl-1,3-oxazolidinyl-5-carbonyl]-10-deacetylbaccatin III 7b; treating the coupled products 7-O-[2-(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3-(2-substituted-2-trialkylsilyl)ethoxy-carbonyl-1,3-oxazolidinyl-S-carbonyl]baccatin III 7a or 7,10-di-0-[2[(haloacyl)]-13-[(4S,5R)-4-aryl-2-substituted-3-(2-substituted-2-trialkylsilyl)ethoxycarbonyl-1,3-oxazolidinyl-5-carbonyl]-10-deacetylbaccatin III 7b with tetraalkylammonium halide in a haloalkane to obtain free amine of structure 8; treating free amine 8 with acid chloride or acid anhydride in the presence of a base in a heterogeneous phase to obtain the intermediates of structure 9; subjecting the intermediates of compound 9 to the deprotection of 2-haloacyl group under mild alkaline condition at ?20 to +40° C. for 6-24 h in the presence of ammonia or aliphatic amines or aromatic amines or their combination to obtain paclitaxel or docetaxel.