2601-07-2Relevant academic research and scientific papers
Oxidative fragmentation of pregna-14,16-dien-20-ones to 14 beta-hydroxyandrost-15-en-17-ones.
Fell, Jennifer D,Heathcock, Clayton H
, p. 4742 - 4746 (2002)
Two methods have been developed for efficient conversion of pregna-14,16-dien-20-ones into 14 beta-hydroxyandrost-15-en-17-ones. One procedure consists of treatment of the ring-D dienone successively with sodium borohydride and singlet oxygen. The reaction is illustrated by the conversion of pregna-14,16-dien-20-one 1 into 14 beta-hydroxyandrost-15-en-17-one 3, via the corresponding allylic alcohol 2. Although this two-step procedure is simple, it provides 3 in relatively low yield, accompanied by a smaller amount of the isomeric 14 alpha-hydroxyandrost-15-en-17-one 6. An alternative one-step conversion is achieved by treatment of dienone 1 with a peroxyacid in the presence of a strong protic acid. This process is illustrated by the two-step conversion of dienone 1 into hydroxy ketone 11 in 51% overall yield (Scheme 5) and by the analogous conversion of dienone 13 into hydroxy ketone 24 in 61% overall yield (Scheme 11).
Steroid compound for treating depression
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Paragraph 0074-0076, (2022/01/04)
The invention discloses a novel compound as shown in a general formula 1, a pharmaceutically acceptable salt and solvate of the novel compound, a stereoisomer comprising mixtures of the novel compound in various proportions and a pharmaceutical composition containing the novel compound. In the formula, R1, R2, R3, R4a, R4b, R5, R6a, R6b, R6c, R6d, R6e, R7a, R7b, R8a, R8b, R9a, R9b, R10a, R10b, ring A and the like have meanings given in the specification. The invention also relates to a preparation method of the compound, and also relates to application of the pharmaceutically acceptable salt, solvate and stereoisomer including mixtures in various proportions of the compound, in particular to application in preparation of medicines for protecting, treating, treating or relieving depression.
Anti-depression steroid compound
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Paragraph 0074-0076, (2021/01/15)
The invention discloses a compound as shown in a general formula I, pharmaceutically acceptable salts and solvates of the compound, stereoisomers containing a mixture of various proportions of the stereoisomers, and a pharmaceutical composition containing the compound. In the formula I, R1, R2, R3, R4a, R4b, R4c, R4d, R6a, R6b, R6c, R6d, R6e, R7a, R7b, R8a, R8b, R9a, R9b, R10a, R10b, X1, X2, X3, X4 and the like are defined in the specification. The invention also relates to a preparation method of the compound, and also relates to an application of the compound, pharmaceutically acceptable salts, solvates and stereoisomers including mixtures of various proportions of stereoisomers, especially an application in preparing medicines for preventing, treating, treating or alleviating depression.
A practical solution for aqueous reactions of water-insoluble high-melting-point organic substrates
Cui, Xiaoxue,Li, Bo,Liu, Tianzhen,Li, Chunbao
supporting information; experimental part, p. 668 - 672 (2012/06/01)
A practical solution to the problem of performing aqueous reactions for very sparingly soluble high-melting-point (VSSHMP) organic substrates has been developed, which entails mechanically stirring a mixture of the substrate, the corresponding reagent(s), water, catalytic Aliquat 336 and sand. When the melting points of the substrates which include steroids, ketones, aldehydes, aromatics and alkaloids are around 200 °C, the reactions can be performed at 20 °C. The substrate solubility can be as low as 1 × 10-10 mol L-1. The Royal Society of Chemistry 2012.
Trimethylchlorosilane/acetyl chloride induced metal mediated chemoselective chlorination of 16-dehydro-20-oxopregnanes
Hazarika,Chowdhury
, p. 145 - 147 (2007/10/03)
Chemoselective chlorination of 16-dehydropregne-nolone acetate (16-DPA) through in situ generation of MnCl4 from a system consisting of MnO2-TMSCl/AcCl has been described.
Process for the preparation of 17β-hydroxy-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone
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, (2008/06/13)
A new process utilizing certain novel intermediates for the preparation of 17β-hydroxy-3-oxo-17α-pregn-4-ene-21-carboxylic acid γ-lactone is described herein. The procedure utilizes readily available and inexpensive sarsasaponin as starting material.
