1352816-81-9

Basic information

• Product Name: 2′-O-(tert-butyldimethylsilyl) cabazitaxel
• Synonyms: 2′-O-(tert-butyldimethylsilyl) cabazitaxel
• CAS NO: 1352816-81-9
• Molecular Weight: 950.209
• Mol File: 1352816-81-9.mol

Chemical Properties

• CAS DataBase Reference: 2′-O-(tert-butyldimethylsilyl) cabazitaxel(CAS DataBase Reference)
• NIST Chemistry Reference: 2′-O-(tert-butyldimethylsilyl) cabazitaxel(1352816-81-9)
• EPA Substance Registry System: 2′-O-(tert-butyldimethylsilyl) cabazitaxel(1352816-81-9)

Safety Data

• Hazardous Substances Data: 1352816-81-9(Hazardous Substances Data)

Upstream product

• 152089-15-1 2’-(tert-butyldimethylsilyl)-7,10-(trichloroethoxycarbonyl)docetaxel 
• 342613-14-3 2'-O-(tert-butyldimethylsilyl)docetaxel 
• 709673-79-0 7,10-methylthiomethyl-10-deacetylbaccatin III 
• 74-88-4 methyl iodide 

Downstream Products

• 183133-96-2 carbazitaxel 

Relevant articles and documents

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.

CABAZITAXEL, RELATED COMPOUNDS AND METHODS OF SYNTHESIS

The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.

CABAZITAXEL, RELATED COMPOUNDS AND METHODS OF SYNTHESIS

The invention provides new cabazitaxel isoserine ester intermediates and new synthetic methods, and a preparation method for the anti-tumour drugs cabazitaxel, docetaxel and paclitaxel from the new cabazitaxel isoserine intermediates.