709673-79-0

Upstream product

• 1402820-66-9 13-acetyl-7,10-methylthiomethyl-10-DAB 
• 110258-96-3 13-acetyl-10-deacetyl baccatin III 
• 92950-44-2 7,13-diacetyl baccatin III 
• 32981-86-5 10-deacetylbaccatin III 
• 67-68-5 dimethyl sulfoxide 
• 162375-26-0 2'-O-(tert-butyldimethylsilyl)-10-deacetylpaclitaxel 
• 114655-02-6 2'-O-(tert-butyldimethylsilyl)paclitaxel 
• 33069-62-4 taxol 
• 709673-63-2 C₅₅H₇₁NO₁₃S₂Si 

Downstream Products

• 709673-74-5 C₃₆H₅₂O₁₀S₂Si 
• 183133-96-2 carbazitaxel 
• 183133-94-0 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β,13α-dihydroxy-7β,10β-dimethoxy-9-oxo-11-taxene 
• 1380584-07-5 1-hydroxy-7β,10β-di-methoxy-9-oxo-5β,20-epoxytax-11-ene-2α,4,13α-triyl 4-acetate 2-benzoate 13-{(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-trethylsilyloxy-3-phenylpropanoate} 

Relevant academic research and scientific papers

Synthesis and biological evaluation of novel cabazitaxel analogues

Cabazitaxel is one of the most recently FDA-approved taxane anticancer agent. In view of the advantages in preclinical and clinical data of cabazitaxel over former toxoids, the synthesis and biological evaluation of novel cabazitaxel analogues were conducted. First, a novel semi-synthesis of cabazitaxel was described. This strategy is concise and efficient, which needs five steps from the 10-deacetylbaccatin III (10-DAB) moiety and a commercially available C13 side chain precursor with a 32% overall yield. Besides, this strategy avoids using many hazardous reagents that involved in the previously reported processes. Then, a panel of cabazitaxel analogues were prepared basing on this strategy. The cytotoxicity evaluations showed that the majority of these cabazitaxel analogues are potent against both A549 and KB cells and their corresponding drug-resistant cell lines KB/VCR, and A549/T, respectively. Further in vivo antitumor efficacies assessment of 7,10-di-O-methylthiomethyl (MTM) modified cabazitaxel (compounds 16 and 19) on SCID mice A549 xenograft model showed they both had similar antitumor activity to the cabazitaxel. Since compound 19 was observed causing more body wight loss on the mice than 16, these preliminary studies suggest 16 might be a potent drug candidate for further preclinical evaluation.

SOLID STATE FORMS OF CABAZITAXEL AND PROCESSES FOR PREPARATION THEREOF

The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer.

Synthesis and biological activity of macrocyclic taxane analogues

A series of paclitaxel analogues possessing a macrocyclic structure between the 7 and 10 positions has been prepared. These compounds possess in vitro activity against a paclitaxel resistant cell line and have in vivo activity comparable to paclitaxel.