Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives
Patent
1984-02-03
1986-01-28
Brown, Johnnie R.
Organic compounds -- part of the class 532-570 series
Organic compounds
Carbohydrates or derivatives
549298, C07H 1520, C07D31744
Patent
active
045672539
ABSTRACT:
One aspect of this invention relates to 2-substituted podophyllotoxin corresponding to the formula: ##STR1## where R.sub.1 is the residue of an electrophile reactant with the precursor enolate, e.g., halogen, i.e., Br, Cl, F and I, lower alkyl (preferably methyl), hydroxyl, --SR.sub.5 where R.sub.5 is lower alkyl, aralkyl or aryl and COOR.sub.6 where R.sub.6 is hydrogen or lower alkyl. Another aspect of this invention relates to 2-substituted etopsides and related compounds corresponding to the formula: ##STR2## where R.sub.1 is as defined above, and where R.sub.2 is: ##STR3## where AcO is acetyl; or ##STR4## where R.sub.3 is hydrogen and R.sub.4 is alkyl, alkenyl, cycloalkyl, 2-furyl, 2-thienyl, aryl, aralkyl, or alkenyl wherein the aromatic ring (preferably phenyl) may be optionally substituted by one or more hydroxyl, alkyl, alkoxy, nitro or halogen; or where each of R.sub.3 and R.sub.4 is alkyl or where each of R.sub.3 and R.sub.4 taken together with the carbon atom to which they are attached signify a saturated cycloaliphatic ring having 5 or 6 carbon atoms; each alkyl, alkenyl or alkoxy above having no more than 10 carbon atoms and each aryl containing no more than 16 carbon atoms excluding substituent on the ring which are defined above. Yet another aspect of this invention relates to novel intermediate compounds. In addition, a further aspect of this invention relates to various methods for preparing the above compounds.
REFERENCES:
patent: 4413120 (1983-11-01), Whistler
Gensler, Walter J., et al., "Nonenolizable Podophyllotoxin Derivatives", Journal of Medicinal Chemistry, 20, No. 5, pp. 635-644, (1977).
Partridge et al., "Jour. of the American Chemical Society", 95, Jan. 2, 1973.
Durst Tony
Freed James C.
Glinski-Oomen Margaret B.
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