65928-58-7Relevant articles and documents
Preparation method of dienogest
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Paragraph 0079; 0083-0103, (2021/01/24)
The invention relates to a preparation method of dienogest. The preparation method comprises the following steps: providing a compound with a structure shown as a formula (II); and carrying out an acidolysis deprotection reaction on the compound shown in the formula (II) in an aqueous fluoboric acid solution to prepare a compound with a structure shown in a formula (I). According to the preparation method of the dienogest, the problems of low purity and dark color of a crude product of an acidolysis deprotection process are fundamentally solved, a production process is greatly simplified, andthe production cost of an enterprise is reduced.
Preparation method of dienogest and method for recovering dienogest from dienogest mother liquor
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Paragraph 0023; 0027-0029, (2021/02/20)
The invention belongs to the technical field of steroid hormone drug preparation, and particularly relates to a preparation method of dienogest and a method for recovering the dienogest from dienogestmother liquor. The preparation method of the dienogest comprises the following steps: dissolving 17 alpha-cyanomethyl-17 beta-hydroxyl-5, 9-androstane diene-3, 17-diketone-3,3-ethyleneketal, adding fluoboric acid, carrying out acidolysis to remove protection, and after the reaction is completed, carrying out treatment to obtain the dinogestrol. The method for recovering the dienogestrol from thedienogestrol mother liquor comprises the following steps: dissolving the dienogestrol with a solvent to obtain the dienogestrol mother liquor, adding perchloric acid or concentrated hydrochloric acid,reacting for a period of time, heating to 45-55 DEG C, concentrating under reduced pressure, removing part of the solvent by concentrating until a solid is separated out, stopping concentrating, cooling, continuing the reaction, and treating to obtain the dienogestrol. The product provided by the invention has high purity and high yield.
Dienogest compound
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Paragraph 0015-0016, (2019/11/04)
The invention provides a dienogest compound. The dienogest compound is characterized in that X-ray diffraction peaks exist when 2*theta is about 12.1+/-0.2, 15.2+/-0.2, 16.6+/-0.2, 18.4+/-0.2, 18.8+/-0.2, 21.9+/-0.2, 23.1+/-0.2 and 24.5+/-0.2.
PROCESS FOR THE PREPARATION OF DIENOGEST SUBSTANTIALLY FREE OF IMPURITIES
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, (2013/03/26)
The present invention provides novel process for preparation and purification of dienogest (I). The present invention provides dienogest (I) substantially free of impurities.
PROCESS FOR THE PREPARATION OF DIENOGEST SUBSTANTIALLY FREE OF IMPURITIES
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Page/Page column 9-10, (2011/11/06)
The present invention provides novel process for preparation and purification of dienogest (I). The present invention provides dienogest (I) substantially free of impurities.
METHOD FOR SYNTHESIS OF DIENOGEST FROM ESTRONE-3-METHYLETHER
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Page/Page column 3, 4, (2010/12/29)
A method for the synthesis of dienogest from 3-methoxy-estra-1,3,5-trien-17-one includes the steps of a) reacting 3-methoxy-estra-1,3,5-trien-17-one with alcohol in the presence of an acid in an organic solvent to form 3-methoxy-17,17-dialkoxy-estra-1,3,5
Process for the preparation of 17alpha-cyanomethyl-17beta-hydroxy steriods
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Page/Page column 3, (2008/12/06)
The invention relates to a process for the preparation of 17α-cyanomethyl-17β hydroxy steroids comprising the reaction of 17-keto steroids with cyanomethyl cerium derivatives. The process is advantageous for the industrial production, since it avoids the use of cyanides and allows to obtain higher yields compared to the use of lithium acetonitrile.
HIGH PURITY 17α-CYANOMETHYL-17β-HYDROXY-ESTRA-4,9-DIENE-3-ONE AND PROCESS FOR THE SYNTHESIS THEREOF
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Page/Page column 9, (2008/06/13)
The invention relates to a new process for the synthesis of high purity 17α- cyanomethyl-17β-hydroxy-estra-4,9-diene-3-one (further on dienogest) of formula (I) from 3-methoxy-17-hydroxy-estra-2,5(10)-diene of formula (V). The invention relates also to th
Pharmaceutical combined preparation, kit and method for hormonal contraception
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, (2008/06/13)
PCT No. PCT/DE96/01192 Sec. 371 Date Jun. 3, 1998 Sec. 102(e) Date Jun. 3, 1998 PCT Filed Jun. 27, 1996 PCT Pub. No. WO97/01342 PCT Pub. Date Jan. 16, 1997The present invention describes a two-stage pharmaceutical combined preparation for hormonal contraception containing at least 30 daily unit doses, which preparation, in its first stage, comprises as hormonal active ingredient a combination of an oestrogen preparation and, in a dose that is at least sufficient to inhibit ovulation, a gestagen preparation, in single stage form and, in the second stage comprises as hormonal active ingredient an oestrogen preparation only, wherein the first stage comprises a minimum of 25 and a maximum of 77 daily discrete or continuous unit doses and the second stage comprises 5, 6 or 7 daily discrete or continuous unit doses, and wherein the total number of daily units is equal to the total number of days of the desired cycle of a minimum of 30 and a maximum of 84 days. This combined preparation, in the form of a monthly pack, which is used for female fertility control, permits as low as possible an oestrogen content in each individual unit dose and also has a low total hormone content per cycle of administration, with high contraceptive reliability, low incidence of follicle development, and satisfactory cycle control with reliable avoidance of intermediate bleeding as well as undesired side effects.