Preparation of 4.beta.- amino podophyllotoxin compounds

Details Preparation of 4.beta.- amino podophyllotoxin compounds Preparation of 4.beta.- amino podophyllotoxin compounds

1992-04-24

1994-08-16

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D30777

Patent

active

053388674

ABSTRACT:
A method of preparing a 4'-0-demethy-4.beta.-NHR podophyllotoxin, where R is an aryl or dialkyl amino alkyl group, is disclosed. The method includes reacting H.sub.2 NR under basic conditions with a mixture of .alpha. and .beta. epimers of 4'-0-demethyl-4-bromo-podophyllotoxin, to form an epimeric mixture of the 4'-0-demethyl-4-NHR-podophyllotoxin compounds, removing acidic impurities which bind to silica gel in a dichloromethane solvent, and crystallizing 4'-0-demethyl-4.beta.-NHR-podophyllotoxin from its .alpha. epimer.

REFERENCES:
patent: 4728740 (1988-03-01), Vyas et al.
patent: 4788216 (1988-11-01), Leander et al.
patent: 5057616 (1991-10-01), Jennings et al.
patent: 5106996 (1992-04-01), Kaneko et al.
patent: 5132322 (1992-07-01), Lee et al.
Lee, K.-H., et al., "Antitumor Agents. 111. New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II," J. Med. Chem. 33:1364-1368 (1990).

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