专利号:US-5089647-A 优先权日:1989-03-09 标题:Method for preparing intermediates for the synthesis of steroid side chains in optically active form 发明人:DELUCA HECTOR F; SCHNOES HEINRICH K; PERLMAN KATO L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:This invention provides a novel method for the preparation of optically active arylalykylsulfone derivatives, having a chiral center in the alkyl moiety in either the (R)- or the (S)-configuration. These optically active sulfones find use in the stereospecific synthesis of steroid or vitamin D compounds having chiral center at either carbon 24 or carbon 25 of the side chain. The method comprises the steps of reacting an optically active sulfinate ester having a chiral center at sulfur with a racemic alkyl Grignard reagent to obtain a mixture of diastereomeric sulfoxides, separating the mixture of diastereomeric sulfoxides, and oxidizing separately each of the diastereomers to obtain the desired optically active sulfone.
专利号:WO-2025108575-A1 优先权日:2023-11-21 标 题:Methods of selective deprotection and synthesis of transhydrindane- skeleton-based compounds 发明人:HUBER FLORIAN MAURITIUS ERASMUS 权利人:ROCHE DIAGNOSTICS GMBH 摘要:The present invention relates to methods of selectively deprotecting a transhydrindane-skeleton-based compound comprising at least two different silyl ether groups. The present invention further relates to methods of synthesizing a Vitamin D molecule and to Vitamin D molecules obtainable by such processes. Furthermore, the present invention relates to a compound according to formula (I) comprising two different silyl ether groups, its use in the synthesis of Vitamin D molecules and to methods of producing such a compound.
专利号:US-2024239742-A1 优先权日:2022-12-29 标 题 :Synthesis of vitamin d3 from cholesterol extracted from fish oil 发明人:VALENCIA OCAMPO JHESUA; MARTINEZ GUTIERREZ WILSON DE JESÚS; VALDEZ CANTILLO WENDY KATHERINE 权利人:VALENCIA OCAMPO JHESUA; MARTINEZ GUTIERREZ WILSON DE JESUS; VALDEZ CANTILLO WENDY KATHERINE 摘要:The present invention provides synthetic methods and preparation of cholecalciferol (vitamin D3) from cholesterol, which is a by-product of the Omega-3 oil production process. According to the invention, dehydro-cholesterol is prepared and subjected to UV radiation (254 nm). Accordingly, two new synthetic alternatives are provided; wherein the first consists of processes of oxidation-reduction of cholesterol to form dehydro-cholesterol and subsequent UV radiation; which route involves six steps (see scheme 1). The second transformation involves the generation of vitamin D3 by means of a bromination method and a photocatalytic reaction using UV radiation; which alternative requires four steps (see scheme 2).
专利号:US-9006412-B2 优先权日:2008-10-06 标题 :Expression vector for pseudonocardia autotrophica 发明人:FUJII YOSHIKAZU; FUJII TADASHI; ARISAWA AKIRA; TAMURA TOMOHIRO 权利人:FUJII YOSHIKAZU; FUJII TADASHI; ARISAWA AKIRA; TAMURA TOMOHIRO; MICROBIOPHARM JAPAN CO LTD; NAT INST OF ADVANCED IND SCIEN 摘要:An expression vector capable of expressing a foreign gene in Pseudonocardia autotrophica ; a transformant of Pseudonocardia autotrophica produced by using the expression vector; a method for producing a protein by using the transformant; a method for producing an active form of vitamin D3 from vitamin D3, which comprises highly expressing a gene encoding an enzyme involved in the synthesis of the active form of vitamin D3 in a transformant by using the expression vector or the transformant; a method for producing 25-hydroxyvitamin D2 from vitamin D2; and a method for producing pravastatin from compactin, which comprises highly expressing a compactin hydroxylase gene in a transformant by using the expression vector or the transformant.
专利号:EP-1494680-B1 优先权日:2002-03-25 标题 :Use of carbon-2-modified-vitamin d analogs to induce the formation of new bone 发明人:DELUCA HECTOR F; PIKE J WESLEY; SHEVDE NIRUPAMA K 权利人:WISCONSIN ALUMNI RES FOUND 摘要:It has been discovered that the 2-carbon-modified derivatives of 1α,25-dihydroxyvitamin D3 specifically stimulate osteoblasts to form new bone. The ability of the 2-carbon-modified vitamin D analogs to stimulate new bone formation suggest that these compounds can be used where synthesis of new bone is required. Thus, these compounds can be used either systemically or locally to stimulate the growth of bone transplants, to increase the rate of fracture healing and thereby reduce the time required for the healing of fractures, the stimulation of bone growth when required for replacement surgery, and also for the growth of bone to implants or other devices required to maintain the skeleton or teeth in the proper positions.
专利号:US-5869472-A 优先权日:1994-07-18 标 题 :Synthesis of 1α-hydroxy vitamin D 发明人:MORIARTY ROBERT M; GUO LIANG; PENMASTA RAJU A 权利人:BONE CARE INT INC 摘要:A method for 1α-hydroxylation of vitamin D compounds using the appropriate vitamin D as the starting material. The method requires no separatory procedures prior to the actual hydroxylation step.
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合成参考文献
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