- Preparation method of ulipristal acetate diketal
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The invention discloses a preparation method of ulipristal acetate diketal. Dihydroxyprogesterone dehydrogenate 1 is used as the raw material to prepare an important intermediate of sterides, namely ulipristal acetate diketal 8; a reaction formula is shown in the attached figure. The preparation method has the advantages that the dihydroxyprogesterone dehydrogenate 1 is used as a starting raw material, seven steps are performed, and the ulipristal acetate diketal with weight total yield rate of 65% or above can be obtained; the reaction is simple, the selectivity is good, and the preparation method is suitable for industrialization production.
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Page/Page column 9-11
(2019/01/11)
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- Steroid compound, preparation method therefor and use of steroid compound
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The invention relates to a steroid compound, a preparation method therefor and use of the steroid compound. The existing methods for preparing 3,3,20,20-bis(ethylenedioxy)-17alpha-hydroxyl-19-norpregna-5(10),9(11)-diene have the problems that starting materials are single, the cost is relatively high, the product quality is poor, the methods are not suitable for industrial production, and the like. The novel steroid compound, the preparation method therefor and the use of the compound, provided by the invention, have the advantages that the steroid compound can be used for preparing 3,3,20,20-bis(ethylenedioxy)-17alpha-hydroxyl-19-norpregna-5(10), 9(11)-diene; and the preparation method is high in yield and product quality, mild in reaction conditions, rich and readily available in raw material and relatively low in cost, thereby facilitating industrial production.
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- ULIPRISTAL ACETATE PREPARATION METHOD AND INTERMEDIATE THEREOF
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A method as well as new intermediates for preparing Ulipristal acetate (a compound I) and a method for preparing the new intermediates are provided. The intermediate in a constitutional formula IV is conductive to reacting with methyl lithium or methyl Grignard reagent, a protective group is easy to be removed after a reaction, side reactions are few, a mid-term treatment is simple, the reagents used are cheap, costs are low and the yield is high, if a compound in a constitutional formula V is obtained by the reaction of a compound in a constitutional formula III and the intermediate in the constitutional formula IV, the yield of a two-step reaction is 75%, a purity is above 98%. wherein R is defined in the specification.
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Paragraph 0036
(2014/09/29)
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- Method for preparing ulipristal acetate and key intermediate thereof
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A method as well as new intermediates for preparing Ulipristal acetate (a compound I) and a method for preparing the new intermediates are provided. The intermediate in a constitutional formula IV is conductive to reacting with methyl lithium or methyl Grignard reagent, a protective group is easy to be removed after a reaction, side reactions are few, a mid-term treatment is simple, the reagents used are cheap, costs are low and a yield is high, if a compound in a constitutional formula V is obtained by the reaction of a compound in a constitutional formula III and the intermediate in the constitutional formula IV, the yield of a two-step reaction is 75%, a purity is above 98%. wherein R is defined in the specification.
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Paragraph 0097
(2014/10/16)
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- METHOD FOR PREPARING 17 alpha-ACETOXY-11beta-(4-N,N-DIMETHYLAMINOPHENYL)-19-NORPREGNA-4,9-DIENE-3,20-DIONE, INTERMEDIATES THEREOF, AND METHODS FOR THE PREPARATION OF SUCH INTERMEDIATES
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Methods for the preparation of the 19-norprogesterone of formula I and its intermediates, in crystalline and amorphous forms.
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- A practical large-scale synthesis of 17α-acetoxy-11β-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione (CDB-2914)
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A new practical synthesis of 17α-acetoxy-11β-(4-N,N-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione (CDB-2914) is described. The synthesis gives easily isolable solids at all steps and is amenable to large-scale process. Copyright (C) 2000 Elsevier Science Inc.
- Rao, Pemmaraju N.,Acosta, C. Kirk,Bahr, Martin L.,Burdett, James E.,Cessac, James W.,Morrison, Paul A.,Kim, Hyun K.
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p. 395 - 400
(2007/10/03)
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- 11 β-substituted progesterone analogs
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A 11β-aryl-19-norprogesterone steroid of the formula: STR1 wherein (i) R1 is H, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, OH, OC(O)CH3, or OC(O)R5, wherein R5 is C2-8 alkyl, C2-8 alkenyl, C2-8 alkynyl or aryl, R2 is H, R3 is H, C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl, R4 is H, CH3, F or Cl, R6 is H, (CH3)2 N, CH3 O, CH3 CO, CH3 S, CH3 SO, CH3 SO2, and X is O or NOCH3 ; or (ii) R1 and R2 taken together are a carbon-carbon bond and R3, R4, R6 and X are as defined above; or (iii) R1 and R3 taken together are --CH2 -- or --N=N--CH2 --, R2 is H and R4, R6 and X are as defined above; or (iv) R2 and R3 taken together are =CH2 and R1, R4, R6 and X are as defined above.
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