- Method and compound for synthetizing reprogestin
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To the synthesis method, dehydropregnenolone is taken as a starting material, carbonyl-protected dehydropregnenolone is prepared, and then a methyl configuration overturning compound is obtained through photo-catalytic reaction and further subjected to deprotection. Hydroxylation and double bond rearrangement reaction yield progestin. The method has the advantages of easily available raw materials, high yield and simple and mild reaction conditions, and is suitable for industrial production of progestin.
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- Method for synthesizing dydrogesterone
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The invention relates to a method for synthesizing a steroid drug dydrogesterone (CAS: 152-62-5). The method comprises the following steps: starting from pregnenolone, carrying out allylic halogenation and elimination to obtain a Pregna-5, 7-dien-3-ol-20-one intermediate; carrying out illumination isomerization to obtain a key intermediate 9 beta, 10 alpha-Pregna-5, 7-dien-3-ol-20-one; then carrying out Oppenauer oxidation (Oppenauer oxidation) to obtain 7-Dehydro-9beta, 10 alpha-progesterone, and finally, carrying out olefin shift isomerization under the action of acid to obtain the final product 6-Dehydro-9beta, 10 alpha-progesterone (a crude drug of dydrogesterone). The method is economical in steps and comprises four conversion steps; the total yield is as high as 16.4%; the raw materials are cheap and easy to obtain, the whole process route is green and safe, the bulk drugs are high in quality, the purity can reach 99.5% or above, and the method is suitable for industrial production.
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Paragraph 0029-0031
(2021/05/19)
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- Production process capable of industrially synthesizing dydrogesterone
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The invention discloses a production process capable of industrially synthesizing dydrogesterone. Easily available progesterone is used as a raw material, and dydrogesterone is prepared through the steps of carbonyl protection, bromination, debromination, photochemical ring-opening reaction, photochemical ring-closing reaction, deprotection and double bond isomerization. The production process hasthe advantages of easily available initial raw materials, and easiness in implementation of each step and higher yield; the production process is simple and convenient to operate, is green and environment-friendly, and can be easily amplified to industrial production.
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- PROCESS FOR PREPARATION OF DYDROGESTERONE
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The present invention relates to process for the preparation of dydrogesterone.
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- 3-Keto-7 α,β-loweralkyl-Δ 5-steroids
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7(α,β)-Loweralkyl-3-keto-Δ 5 -androstanes and 7(α,β)-loweralkyl-3-keto-Δ 5 -pregnanes having anabolic, androgenic, claudogenic, progestational and anti-progestational properties are prepared by reacting 3-keto-4,6-dienic androstanes and pregnanes with organocopper reagents such as dialkyllithium cuprate. The isomerization of these compounds to yield 7(α,β)-loweralkyl-3-keto-Δ 4 -steroids is also described.
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