4-HETERO-16α, 17α-CYCLOHEXANOPREGNANES Russian patent published in 2011 - IPC C07J53/00 C07J73/00 A61P35/00 

FIELD: chemistry.

SUBSTANCE: invention relates to novel 4-oxa- and 4-aza-16α, 17α-cyclohexanopregnanes (4-oxa- and 4-aza-pregna-D'-pentaranes), which can be used n medicine to treat malignant tumours, having general formula I , where X=0 or NR, R=R₁=R₂=R₄=H where R₁+R₃ form a bond. Said compounds are obtained by oxidising ring A 16α, 17α-cyclohexano-progesterone with potassium permanganate and sodium periodate in the presence of sodium carbonate in 5-oxo-A-nor-3,5-secoacid followed by closure of ring A in 4-oxa-16α, 17α-cyclohexanopregn-5-en-20-one while treating with a sodium acetate dehydrating agent in Ac₂O and in 4-aza-16α, 17α-cyclohexanopregn-5-en-20-one using ammonium acetate in acetic acid.

EFFECT: compounds are effective inhibitors of oestrogen-stimulated cell proliferation HeLa.

2 cl, 2 ex, 1 tbl