- Preparation method of vitamin D2
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The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of vitamin D2. Compared with the prior art, the method has the following beneficial effects: the invention provides a technical scheme for synthesizing vitamin D2 through photochemical reaction, thermal isomerization reaction, esterification reaction and saponification reaction by taking ergosterol as an initial raw material, and according to the technical scheme, the effect of high yield of the vitamin D2 is achieved by comprehensively optimizing an organic solvent system in which photochemical reaction is carried out and the temperature of thermal isomerization reaction and washing a saponification product by adopting a proper washing solution.
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Paragraph 0089-0091; 0103-0108; 0120-0125; 0137-0141; 0152
(2021/05/12)
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- Production process of vitamin D2
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The invention discloses a production process of vitamin D2. The process includes the steps of: S1) light irradiation and thermal-isomerization reaction; S2) chromatographic eluting separation; S3) freezing crystallization separation; S4) drying, mixing and packaging. Compared with the prior art, the process is modified in synthetic process conditions, so that the process is improved in productivity and total yield of the product reaches more than 90%. The thermal-isomerization reaction and a pressure-reduced concentration step are combined, so that the process is simplified and is reduced in energy consumption. A synthesis reaction zone and a purifying separation zone are completely separated, so that process maintenance and process management are convenient. In addition, in the purifying process, a chromatographic crystallization method is employed directly instead of a process comprising chromatography, esterification and hydrolytic crystallization in the prior art, so that usage of toxic organic reagents is avoided, and the process is energy-saving, reduces consumption and is environment-friendly. In the production process of the vitamin D2, tail oil and tail materials contain lumisterol, tachysterol and other derivative products, so that it is valuable to deeply research and develop a high-value medicine intermediate.
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Paragraph 0026; 0027; 0028; 0029; 0030; 0031; 0032; 0033
(2017/05/19)
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- Continuous-flow synthesis of activated vitamin D3 and its analogues
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An efficient, two-stage, continuous-flow synthesis of 1α,25-(OH) 2-vitamin D3 (activated vitamin D3) and its analogues was achieved. The developed method afforded the desired products in satisfactory yields using a high-intensity and economical light source, i.e., a high-pressure mercury lamp. In addition, our method required neither intermediate purification nor high-dilution conditions. The Royal Society of Chemistry 2012.
- Fuse, Shinichiro,Mifune, Yuto,Tanabe, Nobutake,Takahashi, Takashi
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experimental part
p. 5205 - 5211
(2012/08/08)
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- (20S)-1alpha-hydroxy-2-methylene-19-nor-vitamin D3 and its uses
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The compound (20S)-1α-hydroxy-2 methylene-19 nor-vitamin D3 and pharmaceutical uses therefor are described herein. This compound exhibits pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the tretment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. This compound also has very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
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- (20S) 1alpha-hydroxy-2alpha-methyl and 2beta-methyl-19-nor-vitamin D3 and their uses
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This invention discloses (20S)-1α-hydroxy-2α-methyl-19-nor-vitamin D3 and (20S)-1α-hydroxy-2β-methyl-19-nor-vitamin D3 and pharmaceutical uses therefor. These compounds exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent and for the treatment of skin diseases such as psoriasis as well as skin conditions such as wrinkles, slack skin, dry skin and insufficient sebum secretion. These compounds also have very significant calcemic activity and therefore may be used to treat immune disorders in humans as well as metabolic bone diseases such as osteoporosis.
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- VITAMIN D DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
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A process for producing hydroxyvitamin D derivatives, characterized by converting a hydrogen atom or atoms at the 2-position, 24-position, 25-position and/or 26-position of a vitamin D into a hydroxyl group or groups in a solution containing a microorganism that belongs to the genus Nocardia, Streptomyces,Sphingomonas or Amycolata which has an ability to hydroxylate vitamin Ds or an enzyme produced by that microorganism, and optionally under the coexistence of a cyclodextrin; and novel vitamin D3 derivatives obtained by that process.
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- Vitamin D3 derivative and treating agent for inflammatory respiratory disease using same
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Compounds expressed by the following general formula (1), 1[wherein, R01 and R02 are each independently a hydrogen atom or a protecting group for a hydroxyl group; Z is one out of the following formulae (1-1), (1-2), (1-3), (1-4) and (1-5)]. 2The compounds can be used as active ingredients of treating agents for inflammatory respiratory diseases, malignant tumors, rheumatoid arthritis, osteoporosis, diabetes mellitus, hypertension, alopecia, acne, psoriasis, dermatitis, hypercalcemia, hypoparathyroidism and metabolic disorder of cartilage.
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- Scalp life conditioner
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The present invention is an improved scalp conditioner for conditions related to flaky and inflamed scalp that are commonly associated with dandruff, seborrhea, psoriasis and burns from the use of alkaline based products. The method involves administering the product to the scalp of the head and gently massaging the scalp. It can be administered several times per week.
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- The modified Julia olefination in vitamin D2 synthesis
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A partial synthesis of vitamin D2 employing fragments derived from a new improved degradation procedure is described. The 7,8-double bond of the vitamin D triene system was synthesised via the modified Julia olefination. The new procedure is more efficient than the classical Julia olefination.
- Blakemore,Kocienski,Marzcak,Wicha
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p. 1209 - 1215
(2007/10/03)
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