Intermediates for the production of epipodophylotoxin and related compounds and processes for the preparation and use thereof
AssigneeBristol-Myers Company
InventorsDolatrai M. Vyas, Paul M. Skonezny
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Abstract
There is provided a novel and efficient stereoselective total synthesis of epipodophyllotoxin and related epipodophyllotoxin compounds of the general formula ##STR1## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy; R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy; and R.sup.5 is hydrogen or a phenol-protecting group; or an acid addition salt thereof. The present invention also provides novel intermediates and processes for the preparation of said intermediates, which are then converted into known antineoplastic agents.
Claims7
A compound of the formula ##STR112## wherein R.sup.1 and R.sup.2 each are independently hydrogen or (lower)alkoxy, or R.sup.1 and R.sup.2, taken together, is methylenedioxy;
- R.sup.3 is hydrogen or a carboxyl-protecting group;
- R.sup.4 and R.sup.6 each are independently hydrogen or (lower)alkoxy;
- R.sup.5 is hydrogen or a phenol-protecting group;
- and
- R.sup.7 is hydrogen, halogen, (lower)alkoxycarbonyl, carboxyl, cyano, trimethylsilyl, phenylsulfonyl or phenoxycarbonyl in which the phenyl ring of R.sup.7 may have one or two substituents independently selected from (lower)alkyl, halogen, (lower)alkoxy and trifluoromethyl;
- or an acid addition salt thereof.
Dependencies are inferred from the claim text.