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US 4,137,230 AGranted
Method for the production of maytansinoids
AssigneeTakeda Chemical Industries, Ltd.
InventorsNaoto Hashimoto, Toyokazu Kishi
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Abstract
Maytansinoid compounds are produced by contacting in the presence of a carbodiimide the compound maytansinol ##STR1## with an acid of the formula: ##STR2## wherein R is lower alkyl, to yield the desired maytansinoids HAVING THE RESULTANT FORMULA: ##STR3## wherein R is lower alkyl. The maytansinoids (I) are both antifungal agents and also antitumor agents. The D-form (with respect to assymetry at the 2'-position) of the maytansinoids (I) represents a new class of compounds having antifungal and antitumor properties.
Claims11
A method of producing a compound of the formula:
- ##STR9## wherein R is lower alkyl which comprises contacting, in the presence of a carbodiimide, the compound maytansinol with an acid of the formula:
- ##STR10## wherein R is lower alkyl.
Dependencies are inferred from the claim text.