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US 5,206,350 AGranted
Synthetic process for the preparation of anti-tumor agent-etoposide
AssigneeShanghai Institute of Pharmaceutical Industry
InventorsZhi-guang Wang, Wei-yong Ma, Chun-nian Zhang
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Abstract
This invention relates to a new synthetic process for the preparation of anti-tumor agent Etoposide (VP16-213). the process, which has shorten reaction route, simple procedure, high yield and low materials cost, therefore facilitates the commercial manufacture of etoposide.
Claims2
A process for preparing the anti-tumor agent etoposide, the process comprising the steps of:
- Step 1:
- condensing 4'-demethyl-epipodophyllotoxin of formula (7):
- ##STR5## with a compound of formula (16):
- ##STR6## at a temperature of 0.degree. to -30.degree. C., in the presence of a boron trifluoride ether catalyst to give a compound of formula (19):
- ##STR7## Step 2--reacting the compound of formula (19) obtained in Step 1 with zinc acetate in methanol at a temperature of 80.degree. to 85.degree. C. for 2 hours, to give etoposide of the formula:
- ##STR8## wherein R.sub.1 in formulae (16) and (19) is C(O)CH.sub.2 Cl.
3 more elements
Dependencies are inferred from the claim text.