- Biocatalytic modifications of ethynodiol diacetate by fungi, anti-proliferative activity, and acetylcholineterase inhibitory of its transformed products
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The fungal transformations of ethynodiol diacetate (1) were investigated for the first-time using Botrytis cinerea, Trichothecium roseum, and R3-2 SP 17. The metabolites obtained are as following: 17α-Ethynyl-17β-acetoxyestr-4-en-3-one-15β-ol (2), 19-nor-
- Nurfazilah Wan Yusop, Sharifah,Imran, Syahrul,Ilham Adenan, Mohd,Ashraf, Kamran,Sultan, Sadia
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- Preparation method of norethindrone acetate (by machine translation)
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The invention discloses a preparation method of norethindrone acetate and belongs to the technical field of drug preparation and processing. The method uses 19 - demethyl -4 - androstenedione as a starting raw material, protects, acetylenically, hydrolyses and esterifies 4 steps to prepare the norethindrone acetate. To the preparation method of the norethindrone acetate, the defects of a traditional process are overcome, reaction conditions are mild, impurities are reduced, overall conversion rate is high, operation is simple and convenient, and the method is suitable for industrial production and has a wide market prospect. (by machine translation)
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- Synthetic method of tibolone
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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.
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Paragraph 0028-0031
(2020/05/01)
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- A 19-nor-4-androstene -3,17-dione method for the preparation of
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The present invention discloses a 19-nor-4-androstene-3,17-dione preparation method without chromium oxidation, wherein 19-hydroxymethyl-4-androstene-3,17-dione is adopted as a raw material, is subjected to 2-iodoxybenzoic acid oxidation and sodium chlorite oxidation in a solvent, and then is subjected to decarboxylation under an acid condition so as to obtain the product 19-nor-4-androstene-3,17-dione. The preparation method of the present invention has characteristics of no requirement of use of the hypertoxic chromium oxidant, high yield, high raw material conversion rate, easy oxidant recycling, and environmental protection, and is widely used for the industrial scale production.
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Paragraph 0040-0043
(2017/04/03)
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- Pharmaceutical combination preparation for hormonal contraception
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The invention provides a pharmaceutical combination preparation with two hormone components in a packaging unit and intended for time-sequential oral administration, comprising a number of daily dosage units physically separate and individually removable in the packaging unit, whereby as a hormonal active ingredient a first hormone component contains in combination an estrogen preparation and in at least a dosage that is sufficient to inhibit ovulation a gestagen preparation, and as a hormonal active ingredient the second hormone component contains only an estrogen preparation, whereby the first hormone component comprises 23 or 24 daily units and the second hormone component comprises 4, 3 or 2 daily units, and between these two hormone components, 2 or 1 active ingredient-free daily units are present or 2 or 1 blank pill days are indicated, and the total number of hormone daily units and the active ingredient-free daily units or the blank pill days is equal to the total number of days of the desired cycle, but at least 28 days in length. This combination preparation is useful for female birth control, and allows for an estrogen content that is as low as possible in each individual dosage unit and also has a low total hormone content per administration cycle, with high contraceptive reliability, low incidence of follicular development, and satisfactory cycle control, with reliable avoidance of intracyclic menstrual bleeding as well as of undesirable side-effects.
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- Pharmaceutical combination preparation for hormonal contraception
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A pharmaceutical combination preparation with two hormone components that are manufactured physically separately in a packaging unit and that are intended for time-sequential oral administration, which in each case consist of a number of daily dosage units that are placed physically separately and are individually removable in the packaging unit. As a hormonal active ingredient, a first hormone component contains in combination an estrogen preparation and, in at least a dosage that is sufficient to inhibit ovulation, a gestagen preparation, and as a hormonal active ingredient the second hormone component contains only an estrogen preparation. The first hormone component comprises 23 or 24 daily units and the second hormone component comprises 4 to 10 daily units. The total number of hormone daily units is equal to the total number of days of the desired cycle, but at least 28 days in length. This combination preparation is used for female birth control, and allows for an estrogen content that is as low as possible in each individual dosage unit and also has a low total hormone content per administration cycle, with high contraceptive reliability, low incidence of follicular development, and satisfactory cycle control, with reliable avoidance of intracyclic menstrual bleeding as well as of undesirable side-effects.
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- Anti-glaucomatous pharmaceutical composition and the process for obtaining them
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The invention relates to the domain of medicinal chemistry. It concerns more particularly that of the preparation of pharmaceutical compositions for ocular use. A subject of the invention is pharmaceutical compositions for ocular use characterized in that they contain at least one selected compound of steroidal structure in combination with or admixed with a pharmaceutically-acceptable, inert carrier or vehicle. The compositions according to the invention are intended to the treatment of glaucoma.
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- Water-soluble steroid compounds
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Beta-cyclodextrin forms a water-soluble complex or inclusion compound with steroid compounds having a molecular structure smaller than the interior cavity in the doughnut-shaped molecular structure of beta-cyclodextrin. The resulting inclusion compounds can be used for a variety of applications including aqueous topical ophthalmic preparations and topical dermatological ointments.
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- Acid- and Base-Catalyzed Isomerization of Androst-5-ene-3,17-dione and 17α-Ethynyl-17β-hydroxy-5-estren-3-one
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Isomerization of androst-5-ene-3,17-dione (1) to androst-4-ene-3,17-dione (2) and of 17α-ethynyl-17β-hydroxy-5-estren-3-one (3) to 17α-ethynyl-17β-hydroxy-4-estren-3-one (4) is kinetically general acid-base catalyzed; 1 is more reactive than 3.Deuterium solvent kinetic isotope effects, k(H2O)/k(D2O), of ca.6 for tertiary amine catalyzed isomerization indicate rate-determining protonation of dienolate ions.The greater reactivity of 1 than 3, catalyzed by tertiary amines, is probably due to a greater concentration of the 1 dienolate ion than of the 3 dienolate ion.Ethanolamine, but not tris(hydroxymethyl)aminomethane, catalyzes isomerization of 1 and 3 via Schiff-base formation.Curvilinear pseudo-first-order plots for isomerization of 1 and 3 catalyzed by DCl/D2O indicate that partitioning of dienols is kinetically important.
- Perera, S. K.,Dunn, W. A.,Fedor, L. R.
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p. 2816 - 2821
(2007/10/02)
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- Synthesis of gon-4-enes
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1. A therapeutic composition having progestational activity comprising as active ingredient a 17-aliphatic carboxylic acid ester of 17α-ethynyl-18-methyl-19-nortestosterone and a pharmaceutical carrier for said compound.
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- Synthesis of 13-alkyl-gon-4-ones
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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.
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- Novel N-nitroso compounds, compositions containing such compounds, processes for their preparation and methods of treatment therewith, and novel intermediates
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This invention relates to novel N-halogenoalkyl-N-nitroso carbamates and N 4 halogenalkyl-N 4 -nitroso allophanates of steroid compounds, having an anti-tumor activity, and to the preparation thereof. The invention is also concerned with pharmaceutical compositions containing the said compounds, and methods of treatment therewith.
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