NEW MATERIAL: A compound of formula I [R is H, an alkyl, an alkenyl, an alkynyl, an acyl, an aryl, etc.; X is O, N-O-R1 (R1 is an alkyl), formula II (RA and RB are each H, a halogen, etc.), (H,H) or formula III; Y is formula III (excluding X), formula IV (RC is H, an alkyl, etc.), formula V ((q) is 1-3); W is H, an alkyl, an alkylthio or an arylthio; Z is H or an alkyl; (n) is 0-2] and its salt.
EXAMPLE: 10β-[2-(Methyltio)ethyl]-estra-4,9(11)-diene-3,17-dione.
USE: The compound exhibits aromatase specific activity and is suitable for use in treatment of hormone-dependent diseases, especially estrogen-dependent diseases.
PROCESS: For example, a compound of formula VI (K and K' are each a protected keto group; Alk is an alkyl) is reduced, and the OH group in the resultant product is converted into SH group, then treated with a reactive derivative of the group R to give a compound of formula VII. Treatment of the product with a deblocking agent gives a corresponding compound of formula I.
DOMINIKU RUSUYUISU