孕烯醇酮醋酸酯置于platinum(Iv) Oxide 氢氧化钾,氢气,Pyridinium Chlorochromate体系中,用 乙醇,二氯甲烷 作为反应溶剂,25.0 °C,607.95 Kpa 条件下,反应 7.25H,反应生成 别孕烯醇酮 参考文献:Oxygen-Functionalization Of C13-Angular Methyl Group In Pregnane Steroid By Means Of Intramolecular Carbonyl-Mediated Anodic Oxidation. 标题:Oxygen-Functionalization Of C13-Angular Methyl Group In Pregnane Steroid By Means Of Intramolecular Carbonyl-Mediated Anodic Oxidation. 摘要:对3β-醋酸酯-5α-孕烯-20-酮及其四-O-醋酸β-D-葡萄糖苷衍生物中c13-角甲基的氧官能化已通过在类固醇骨架中c20-羰基残基介导的阳极氧化实现. DOI:10.1248/cpb.40.1143
专利号:US-6333317-B1 优先权日:1997-03-28 标 题:Regulation of amyloid precursor protein (APP) expression by administration of an estrogenic compound 发明人:LEE ROBERT K K; WURTMAN RICHARD J 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:It has been discovered that lipophilic hormones that interact with cytosolic or nuclear receptors regulate APP expression and synthesis, through modification of APP mRNA stability and/or regulation of APP gene transcription and translation activities. These studies demonstrate that the treatment of brain cells with estrone or 17β-estradiol results in a reduction in the level of APP holoprotein expression, without a concomitant change in the total level of cell protein. The reduction in the level of APP holoprotein caused by estrone or 17β-estradiol is also expected to reduce the production of neurotoxic APP fragments. In as much as estrogen deficiency in postmenopausal women is associated with a higher incidence of Alzheimer's disease, this discovery opens the possibility that estrogen therapy may prevent some of the neurodegenerative and cognitive changes associated with Alzheimer's disease, aging and other disease conditions associated with such neurodegenerative and cognitive decline.
专利号:CA-2934466-A1 优先权日:2013-12-20 标题 :Synthesis of ent-progesterone and intermediates thereof
专利号:CA-2961628-A1 优先权日:2014-09-17 标题:Synthesis of ent-progesterone and intermediates thereof
专利号:US-2016016988-A1 优先权日:2013-03-15 标题:Synthesis of ent-progesterone and intermediates thereof
专利号:AU-2014233156-A1 优先权日:2013-03-15 标 题:Synthesis of ent-progesterone and intermediates thereof
专利号:AU-2014364850-A1 优先权日:2013-12-20 标 题 :Synthesis of ent-progesterone and intermediates thereof
1: Singhal M, Modi N, Bansal L, Abraham J, Mehta I, Ravi A. The Emerging Role of Neurosteroids: Novel Drugs Brexanalone, Sepranolone, Zuranolone, and Ganaxolone in Mood and Neurological Disorders. Cureus. 2024 Jul 31;16(7):e65866. doi: 10.7759/cureus.65866. 2: Cadeddu R, Van Zandt M, Santovito LS, Odeh K, Anderson CJ, Flanagan D, Nordkild P, Pinna G, Pittenger C, Bortolato M. Prefrontal allopregnanolone mediates the adverse effects of acute stress in a mouse model of tic pathophysiology. Neuropsychopharmacology. 2023 Aug;48(9):1288-1299. doi: 10.1038/s41386-023-01603-6. Epub 2023 May 17. 3: Tiranini L, Nappi RE. Recent advances in understanding/management of premenstrual dysphoric disorder/premenstrual syndrome. Fac Rev. 2022 Apr 28;11:11. doi: 10.12703/r/11-11.
合成参考文献
参考文献:10.1186/1471-2148-8-103 摘要:Ekins S, Reschly EJ, Hagey LR, Krasowski MD. Evolution of pharmacologic specificity in the pregnane X receptor. BMC Ecology and Evolution. 2008 Apr 02;8(1):103. doi: 10.1186/1471-2148-8-103. 摘要:Milata, V.; Rádl, S.; Voltrová, S., Science of Synthesis, (2008) 32, 625.