Estradiol derivative-alkylating agent conjugate with reduced hor

Details Estradiol derivative-alkylating agent conjugate with reduced hor Estradiol derivative-alkylating agent conjugate with reduced hor

1996-08-05

1997-05-27

Prior, Kimberly J.

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

Organic compounds

Cyclopentanohydrophenanthrene ring system containing

552614, 552618, 552626, C07J 7500

Patent

active

056333935

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.

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patent: 4938897 (1990-07-01), Asano et al.
patent: 5354745 (1994-10-01), Tamura et al.
Morrison & Boyd, Organic Chemistry, 4th ed, pp. 787, 798-799, 827-829, 820-825 and 831 & 837-838 (1983).
Pharmazie 38 (1983), H. 7 pp. 445-448 Mohsen et al Steroidal Derivatives "Synthesis and in vitro Anabolic and Catabolic Properties of a New Group of Steroidal Alkylating Agents".
J. Steroid Biochem. vol. 29, No. 6, pp. 657-664, 1988 Qian et al "Synthesis and Biological Activity of 17.beta.-Substituted Estradiol".

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