2205-78-9Relevant articles and documents
Synthetic method of tibolone
-
, (2020/05/01)
The intention relates to a synthesis method of tibolone, which specifically comprises the following steps: 1) ethynylation reaction: introducing acetylene gas into an acidic decarboxylate (I) toluenesolution as a raw material, and reacting to obtain norethindrone (II); 2) acylation reaction: adding acetic anhydride and an acid-binding agent into the norethindrone (II) obtained in the step 1), controlling the room temperature, dropwise adding acetyl chloride, and stirring to react for 6 hours until the raw material is completely reacted to obtain an acylate (III); 3) carrying out debrominationreaction on the acylate to obtain 4, 6-diene norethindrone acetate (V); 4) methylation reaction: adding an ether solvent into the 4, 6-diene norethindrone acetate (V), cooling to -10 to 30 DEG C, dropwisely adding a methylation reagent, controlling the temperature at 0-5 DEG C, and stirring to react until the raw material reaction is complete, thereby obtaining 7alpha-methyl norethindrone acetate(VI); 5) transposition reaction: reacting the 7 alpha- methyl norethindrone acetate (VI) to obtain a transposition substance (VII) wet product, and 6) hydrolysis reaction: reacting the transpositionsubstance (VII) to obtain the tibolone.
Synthesis of 13-alkyl-gon-4-ones
-
, (2008/06/13)
The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.
