Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol comprising i) the preparation of a compound of general formula (II) by reacting a compound of general formula (I) in one or more steps to a compound of general formula II wherein R1 is a C1-C10 alkyl, alkenyl or aryl group; —Cl, —Br, —I, —F; —CN; —OH; or a —OR2, —O(CO)R2 or —R2-OH group, wherein R2 is an alkyl or alkylene group having 1-6 C atoms; and the bonding between atoms 9 and 10 is a single or a double bond. ii) aromatization of the compound of general formula II to a compound of general formula III wherein R1 and R2 have the above defined meanings; and iii) optionally, reduction of the compound of general formula III to a compound of general formula IV wherein R1 and R2 have the above defined meanings. Furthermore the invention provides several novel compounds, which can be intermediates in the above process, and processes to prepare these novel compounds.

Abstract: The invention provides a process for the preparation of 2-substituted-derivatives of estrone and estradiol. The invention also provides several novel compounds, which can be intermediates in the process, and processes to prepare these novel compounds. The invention also provides 2-alkoxy-estrone, 2-alkoxy-estradiol or mixtures thereof essentially free from other estrogenic intermediates.

Abstract: The invention relates to a process for the preparation of 7?-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C?CH; R2 is (CH2)nOH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Grignard reagent CH3MgX, X being a halogen, to the 4,6-unsaturated 3-ketosteroid of formula II, wherein R1 and R2 are as previously defined, comprising protecting the hydroxy group of the steroid of formula II with a trialkylsilyl group, followed by treating the hydroxy protected steroid with the Grignard reagent. The process of the invention is useful for the production of pharmacologically interesting steroids.

Abstract: The invention relates to a process for the preparation of 7?-methyl hydroxy steroids of the formula I wherein R1 is hydrogen, methyl or C?CH; R2 is (CH2)nOH, wherein n is 0, 1 or 2; by a copper mediated 1,6-conjugate addition of a Grignard reagent CH3MgX, X being a halogen, to the 4,6-unsaturated 3-ketosteroid of formula II, wherein R1 and R2 are as previously defined, comprising protecting the hydroxy group of the steroid of formula II with a trialkylsilyl group, followed by treating the hydroxy protected steroid with the Grignard reagent. The process of the invention is useful for the production of pharmacologically interesting steroids.