Synthesis of danazol derivatives and steroidal-3-oxo-2 alpha-carbonitriles
Shi, J.F.; Xu, F.; Liao, Q.J.
Yao Xue Xue Bao 23(2): 148-151
1988
ISSN/ISBN: 0513-4870 PMID: 3188923 Document Number: 319716
Synthesis of danazol analogues involved transformation of 3-keto-steroids (Ia.apprx.c) into 2-hydroxymethylene steroids (IIa.apprx.c) and subsequent cyclization to steroidal (2, 3 d) isoxazoles (IIIa.apprx.c), Further treatment with sodium methoxide gave the corresponding steroidal-3-oxo-2.alpha.-carbonitriles (IVa.apprx.c). The binding ability of (IIIa.apprx.c) and (IVa.apprx.c) to progesterone receptor were examined and (IIIc) was found to be two times as active as danazol.
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