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US 5,633,393 AGranted
Estradiol derivative-alkylating agent conjugate with reduced hormonal activity, process for preparing the same, compounds useful for the preparation thereof, and growth inhibiting compositon containing the conjugate or estradiol derivative.
AssigneeKureha Kagaku Kogyo Kabushiki Kaisha
InventorsKoichi Niimura, Takako Kawabe, Tsutomu Wada, Tsuyoshi Saitoh, Kenji Bannai
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Abstract
Conjugates of the formula ##STR1## are prepared by reacting an estradiol derivative with a compound of the formula: ##STR2## in the presence of thionyl chloride or a metal hydride at -30.degree. to 150.degree. C. for 3 minutes to 48 hours and then recovering and purifying the product.
Claims1
A process for preparing the conjugate represented by the formula (I):
- ##STR11## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy;
- R.sup.2 is acyl or benzyl;
- R.sup.3 is methylene;
- m is an integer of 1 to 3;
- n is an integer of 0 to 3;
- and X is hydroxy or halogen,
- which comprises (a) reacting an estradiol derivative of the formula (II):
- ##STR12## wherein R.sup.1 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy;
- R.sup.2 is acyl or benzyl;
- m is an integer of 1 to 3;
- n is an integer of 0 to 3;
- and X is hydroxy,
- with a compound of the formula (III):
- ##STR13## wherein R.sup.4 is methyl halide group and X is halogen or hydroxy, in the presence of metal hydride at a temperature of -30.degree. to 150.degree. C. for 3 minutes to 48 hours, and (b) recovering and purifying the conjugate of formula (I).
11 more elements
Dependencies are inferred from the claim text.