10BETA-ALKYNYLESTRENE DERIVATIVES AND PROCESS FOR THEIR PREPARATION

摘要

6-Substituted 10 beta -alkynylestrene derivatives of formula (I): …… wherein… X is hydrogen, C1-C4 alkyl or halogen;… n is zero, 1 or 2;… Y is an oxo group or a methylene group;… the symbol @ indicates a single bond or a double bond;… R1 is halogen, azido or a group …… wherein each of R3 and R4 is, independently, hydrogen or C1-C4 alkyl, or R1 may be divalent and is a C1-C6 alkylidene group; and R2 is hydrogen or, when R1 is halogen, R2 may also be the same halogen as R1,… and the pharmaceutically acceptable salts thereof; are aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors and prostatic hyperplasia.