52 results about "Pregnene" patented technology

The invention relates to a method for preparing a steroidal drug intermediate. The method comprises the steps that microbial conversion is conducted on a first compound with Nocardioides simplex to obtain the steroid drug intermediate, the first compound is shown as a formula I, the steroidal drug intermediate is as shown in a formula II, and in the formula I and the formula II, R is H, a halogenatom, an alkyl group, an alkoxy group, a hydroxyl group or a phenyl group. The method selects 4, 9 (11)-pregnant-17-hydroxy group-3,20 dioxin-21-acetate as a substrate, uses only the Nocardioides simplex for biotransformation, dehydrogenation at position 1,2 and hydrolysis of acetate at position 21 are simultaneously conducted on the substrate, 1,4,9 (11)-pregnene-17,21-diol-3,20-dione is obtained, products formed through transformation are mainly the 1,4,9(11)-pregnene-17,21-diol-3,20-dione, the proportion of by-products is low, the purified products are white or off-white crystals, relativesubstrate weight yield is 75%-85%, a target product yield is high, after a HPLC analysis, the purity is >=99%, and external standard content is 98%.

The invention relates to a synthesis method and main intermediates of pregnene-1,4,9 (11),16 (17)-tetraenol-3, 20-diketone. The synthesis method sequentially comprises the following steps of reacting a second intermediate and tosylmethyl isocyanide in an organic solvent at the temperature of lower than 35 DEG C below zero to generate a third intermediate; reacting the third intermediate and a methylated reagent in an organic solvent at the temperature of 70-90 DEG C, and then, removing methyl ether protecting groups and tosylmethyl isocyanide under the action of an acid to obtain a fourth intermediate; and reacting the fourth intermreidate under the action of 3-ketosteroid-1-dehydrogenase to generate pregnene-1,4,9 (11),16 (17)-tetraenol-3, 20-diketone. Raw materials of pregnene-1,4,9 (11),16 (17)-tetraenol-3, 20-diketone are cheap and available; the yield of pregnene-1,4,9 (11),16 (17)-tetraenol-3, 20-diketone is relatively high; a C17-position side chain is introduced by using tosylmethyl isocyanide, so that acetone cyanohydrin serving as a highly-toxic reagent is prevented from being used; and the synthesis method is safe, environment-friendly and suitable for industrial production.

The invention discloses a preparation method of dutasteride (N-(2,5-di(trifluoromethyl)phenyl)-4-aza-5alpha-androstane-1-ene-3-keto-17beta-formamide, I). The preparation method comprises the following steps that: pregnene ketonic acid (II) is taken as a raw material to convert carboxylic acid to amide through amidation to prepare androstane-4-ene-3-keto-17beta-formamide (III); the compound (III) is subjected to oxidative ring opening and ammonolysis cyclization to prepare 4-aza-androstane-5-ene-3-keto-17beta-formamide (IV); the compound (IV) is subjected to reductive hydrogenation reaction to generate 4-aza-5alpha-androstane-3-keto-17beta-formamide (V); the compound (V) is subjected to oxidative dehydrogenation to generate 4-aza-5alpha-androstane-1-ene-3-keto-17beta-formamide (VI); and the compound (VI) and 2,5-di(trifluoromethyl phenylamine) (VII) carry out amine exchange reaction in the presence of a catalyst to prepare dutasteride (I). The preparation method has the advantages of concise process, easiness in obtaining raw materials and controllable quality, and is suitable for industrial production.