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1. 发明授权

US5382732A 2,5-bis(1,1-dialkoxy-2-propyl)-2,5-dihydrofurans, the preparation thereof and the use thereof for the preparation of carotenoids 失效
标题翻译： 2,5-双（1,1-二烷氧基-2-丙基）-2,5-二氢呋喃，其制备方法及其用于制备类胡萝卜素
公开(公告)号：US5382732A
公开(公告)日：1995-01-17
申请号：US67618
申请日：1993-05-27
申请人： Juergen Frank , Udo Rheude , Bernhard Schulz , Joachim Paust , Eckhard Hickmann
发明人： Juergen Frank , Udo Rheude , Bernhard Schulz , Joachim Paust , Eckhard Hickmann
IPC分类号： B01J27/128 , B01J27/138 , C07B61/00 , C07C47/21 , C07C403/24 , C07D307/28 , C07C403/06
CPC分类号： C07C403/24 , C07D307/28
摘要： A process of preparing symmetric C.sub.40 -carotenoids by reacting a C.sub.15 -triphenylphosphonium salt of the formula ##STR1## and a 2,5-bis(1,1-dialkoxy-2-propyl)-2,5-dihydrofuran to form a reaction product containing a diacetyl and a triphenylphosphonium salt, adding a strong base to the reaction product to convert the triphenylphosphonium salt to a carbenium ion, hydrolyzing the diacetyl to a dialdehyde, subjecting the dialdehyde and the carbenium ion to a Wittig reaction to prepare a Wittig reaction product, and converting the Wittig reaction product to the C.sub.40 -carotenoid by acid treatment.
摘要翻译：通过使式（I）所示的C 15 - 三苯基鏻盐与2,5-双（1,1-二烷氧基-2-丙基）-2,5-二氢呋喃反应制备对称C 40 - 类胡萝卜素的方法，以形成反应产物含有二乙酰基和三苯基鏻盐，向反应产物中加入强碱以将三苯基鏻盐转化为碳鎓离子，将二乙酰基水解成二醛，使二醛和碳鎓离子进行维t希反应以制备Wittig反应产物，并通过酸处理将维蒂希反应产物转化为C40-类胡萝卜素。

2. 发明授权

US4175205A Process for the preparation of vitamin A from sulphones 失效
标题翻译：从sulphones制备维生素A的过程
公开(公告)号：US4175205A
公开(公告)日：1979-11-20
申请号：US818871
申请日：1977-07-25
申请人： Jean-Pierre Decor
发明人： Jean-Pierre Decor
IPC分类号： C07B61/00 , A61K20060101 , A61K31/07 , B01J31/00 , B01J31/02 , C07C20060101 , C07C67/00 , C07C69/14 , C07C69/24 , C07C401/00 , C07C403/00 , C07C403/06 , C07C403/12 , C07C403/22
CPC分类号： C07C403/08 , C07C403/12 , C07C403/22 , C07C2101/16
摘要： Vitamin A alcohol and its lower alkanoic esters are prepared by desulphonation of corresponding sulphones with a solid potassium alcoholate of a primary or secondary lower alcohol at 10.degree. to 50.degree. C. in an anhydrous liquid hydrocarbon.
摘要翻译：维生素A醇及其低级链烷酸酯是通过在10至50℃的无水液体烃中用相同的醇与固体的伯醇或二级低级醇的醇化物脱磺酸来制备的。

3. 发明授权

US6150561A Method of making carotenoids 有权
标题翻译：制备类胡萝卜素的方法
公开(公告)号：US6150561A
公开(公告)日：2000-11-21
申请号：US148088
申请日：1998-09-04
申请人： Paul Kreienbuhl , Peter Rudin , Werner Rudolph
发明人： Paul Kreienbuhl , Peter Rudin , Werner Rudolph
IPC分类号： C07B37/04 , C07C1/34 , C07C11/02 , C07C11/21 , C07C45/51 , C07C67/31 , C07C67/343 , C07C69/347 , C07C69/602 , C07C403/02 , C07C403/06 , C07C403/16 , C07C403/20 , C07C403/24 , C07C45/00
CPC分类号： C07C403/24 , C07C1/34 , C07C403/14 , C07C403/20 , C07C45/515 , C07C67/343 , C07C2101/16
摘要： A widely applicable process for the manufacture of carotenoids by a Wittig reaction comprises carrying out the Wittig reaction in a polar reaction medium in a manner such that neither the reactants nor the thus-manufactured carotenoid are significantly dissolved in the reaction medium. An especially suitable reaction medium is a polar, toxicologically harmless solvent which remains monophasic on the addition of water in an amount up to about 30 vol. % and which permits the triarylphosphine oxide which is formed to dissolve well. Lower alcohols and acetone, as sole solvents or as mixtures with one another and/or with water, are especially suitable as the polar reaction medium. This process permits the use of much more concentrated reaction mixtures, simplifies the regeneration of the solvent and generally the reaction procedure, and avoids toxicologically objectionable solvents such as halogenated hydrocarbons.
摘要翻译：用于通过Wittig反应制造类胡萝卜素的广泛应用的方法包括在极性反应介质中进行Wittig反应，使得反应物和由此制得的类胡萝卜素都不会明显地溶解在反应介质中。特别合适的反应介质是极性，毒理学上无害的溶剂，其在加入至多约30体积的量时保持单相。％，这使得形成的三芳基氧化膦容易溶解。作为唯一溶剂或作为彼此和/或与水的混合物的低级醇和丙酮特别适合作为极性反应介质。该方法允许使用更浓缩的反应混合物，简化了溶剂的再生和通常的反应过程，并避免了毒理学上令人反感的溶剂如卤代烃。

4. 发明授权

US5663459A Intermediates for the preparation of vitamin A and carotenoids and process for their preparation 失效
标题翻译：用于制备维生素A和类胡萝卜素的中间体及其制备方法
公开(公告)号：US5663459A
公开(公告)日：1997-09-02
申请号：US473226
申请日：1995-06-07
申请人： Hugues Bienayme , Pierre Meilland
发明人： Hugues Bienayme , Pierre Meilland
IPC分类号： C07C33/14 , C07C49/21 , C07C403/00 , C07C403/06 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/14 , C07C403/16 , C07C403/20
CPC分类号： C07C403/14 , C07C403/02 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/16 , C07C403/20 , C07B2200/09 , C07C2101/16
摘要： The present invention relates to novel intermediates for the preparation of vitamin A and carotenoids corresponding to the formula (II): ##STR1## in which A represents a hydrogen or an alkyl, alkenyl or alkoxy group containing 1 to 4 carbon atoms, and X represents a carbon atom, and to a process for their preparation and their use, and further relates to compounds for preparing intermediates of formula (II) corresponding to the formula (III): ##STR2## in which R represents a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, an alkenyl group having 2 to 10 carbon atoms, an alkylcarbonyl, alkenylcarbonyl, alkoxyalkyl or alkoxyalkenyl group in which the alkyl groups have 1 to 10 carbon atoms and the alkenyl groups have 2 to 10 carbon atoms, each of said groups being linear or branched and each being substituted or unsubstituted.
摘要翻译：本发明涉及用于制备对应于式（II）的维生素A和类胡萝卜素的新型中间体：其中A表示氢或含有1至4个碳原子的烷基，烯基或烷氧基，并且X表示碳原子，并涉及其制备方法及其应用，还涉及制备对应于式（III）的式（II）的中间体的化合物：其中R表示氢原子，碳原子数1〜10的烷基，碳原子数2〜10的烯基，烷基，碳原子数1〜10的烷基羰基，链烯基羰基，烷氧基烷基或烷氧基烯基，烯基具有2〜 10个碳原子，所述基团各自为直链或支链的，各自为取代或未取代的。

5. 发明授权

US5449844A Intermediates for preparing vitamins A and E and carotenoids 失效
标题翻译：制备维生素A和E以及类胡萝卜素的中间体
公开(公告)号：US5449844A
公开(公告)日：1995-09-12
申请号：US982675
申请日：1992-11-27
申请人： Jean-Erick Ancel , Bienayme, Hugues , Lucette Duhamel , Pierre Duhamel
发明人： Jean-Erick Ancel , Bienayme, Hugues , Lucette Duhamel , Pierre Duhamel
IPC分类号： C07C29/44 , C07C33/44 , C07C45/51 , C07C45/65 , C07C47/21 , C07C47/24 , C07C47/267 , C07C49/203 , C07C49/227 , C07C49/242 , C07C49/255 , C07C323/15 , C07C391/02 , C07C403/06 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/14 , H01R13/639 , C07C43/00
CPC分类号： C07C403/22 , C07C391/02 , C07C403/08 , C07C403/12 , C07C403/14 , C07C403/16 , C07C45/511 , C07C45/513 , C07C45/65 , C07C47/21 , C07C47/24 , C07C49/203 , C07C2101/16
摘要： The present invention relates to a new method of condensing polyenic compounds wherein a compound having the formula III ##STR1## is condensed with a compound having the formula IV ##STR2## under the influence of a Lewis acid or a protic acid. R.sub.1 through R.sub.7 represent alkyl or alkenyl groups, A' is preferably chlorine, B is preferably a hydroxyl group, and n' is 0 to 10. The invention also relates to novel intermediates for use in the preparation of Vitamins A and E produced by means of the new method.
摘要翻译：本发明涉及一种缩合多元化合物的新方法，其中具有式III的化合物（III）在路易斯酸或质子的影响下与具有式IV的化合物（IV）缩合酸。 R1至R7表示烷基或烯基，A'优选为氯，B优选为羟基，n'为0至10.本发明还涉及用于制备维生素A和E的新型中间体的新方法。

6. 发明授权

US5276209A Preparation of polyenes 失效
标题翻译：多烯的制备
公开(公告)号：US5276209A
公开(公告)日：1994-01-04
申请号：US914128
申请日：1992-07-17
申请人： Hagen Jaedicke , Klaus Kaiser , Manfred Hamm
发明人： Hagen Jaedicke , Klaus Kaiser , Manfred Hamm
IPC分类号： C07C403/06 , C07C45/60 , C07C67/02 , C07C403/00 , C07C403/10 , C07C403/12 , C07C403/14 , C07C403/20 , C07C403/22 , C07D319/06
CPC分类号： C07C403/12 , C07C403/08 , C07C403/14 , C07C403/22 , C07C45/60 , C07D319/06 , C07C2101/16
摘要： An improved process for the preparation of polyenes by the Julia reaction comprises carrying out the allylation of the anion of an allyl aryl sulfone generated a strong base, and the elimination of arylsulfinic acid to form a double bond in the same inert polar solvent which is immiscible with water, preferably in a ketone of the formula IR.sup.1 --CO--R.sup.2 (I)where R.sup.1 and R.sup.2 are each straight-chain or branched alkyl of 2 to 4 carbons, or R.sup.1 and R.sup.2 together are tetramethylene or pentamethylene. The process is particularly important for the preparation of vitamin A derivatives. In the preparation of vitamin A aldehyde, for example, it is advantageous to use the same alkali metal alcoholate as strong base in both stages so that the conversion can be carried out as one-pot reaction.
摘要翻译：通过Julia反应制备多烯的改进方法包括进行产生强碱的烯丙基芳基砜的阴离子的烯丙基化，以及消除芳基亚磺酸在与不混溶的相同惰性极性溶剂中形成双键其中R1和R2分别是2至4个碳的直链或支链烷基，或者R1和R2一起是四亚甲基或五亚甲基。该方法对于制备维生素A衍生物尤为重要。在维生素A醛的制备中，例如，在两个阶段中使用相同的碱金属醇盐作为强碱是有利的，因此转化可以作为一锅反应进行。

7. 发明授权

US4942262A Process for producing vitamin A or its carboxylic acid esters 失效
标题翻译：生产维生素A或其羧酸酯的方法
公开(公告)号：US4942262A
公开(公告)日：1990-07-17
申请号：US368800
申请日：1989-06-20
申请人： Toshiki Mori , Shigeaki Suzuki , Takashi Onishi
发明人： Toshiki Mori , Shigeaki Suzuki , Takashi Onishi
IPC分类号： C07C20060101 , C07C317/14 , C07C403/06 , C07C403/08 , C07C403/12
CPC分类号： C07C403/08 , C07C403/12 , C07C403/22 , C07C2101/16
摘要： The invention provides a process for producing vitamin A or its carboxylic acid ester by treating inexpensive and readily available industrial starting materials with potassium hydroxide which is widely employed industrially and is inexpensive.

8. 发明授权

US4739098A Ethynylphenyl-containing retinoic acid derivatives 失效
标题翻译：含乙炔基苯基的视黄酸衍生物
公开(公告)号：US4739098A
公开(公告)日：1988-04-19
申请号：US910096
申请日：1986-09-22
申请人： Roshantha A. S. Chandraratna
发明人： Roshantha A. S. Chandraratna
IPC分类号： A61K31/015 , A61K20060101 , A61K31/045 , A61K31/07 , A61K31/075 , A61K31/085 , A61K31/11 , A61K31/16 , A61K31/165 , A61K31/185 , A61K31/19 , A61K31/215 , A61K31/235 , A61P17/00 , A61P27/16 , A61P29/00 , A61P37/00 , C07C20060101 , C07C13/00 , C07C13/16 , C07C13/20 , C07C15/00 , C07C15/50 , C07C33/38 , C07C39/23 , C07C43/168 , C07C47/238 , C07C47/548 , C07C57/00 , C07C57/48 , C07C63/00 , C07C63/33 , C07C63/66 , C07C67/00 , C07C69/00 , C07C69/606 , C07C69/612 , C07C69/614 , C07C69/618 , C07C69/76 , C07C69/78 , C07C233/65 , C07C401/00 , C07C403/00 , C07C403/02 , C07C403/06 , C07C403/14 , C07C403/20 , C07C403/24
CPC分类号： C07C403/14 , C07C403/08 , C07C403/10 , C07C403/12 , C07C403/20 , C07C2101/16
摘要： Retinoid-like activity is exhibited by compounds of the formula ##STR1## where n is 0-5 and A is H, lower alkyl, or --COOH or ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative, or --CHO or an acetal derivative, or a pharmaceutically acceptable salt.

9. 发明授权

US09388130B2 Retinal derivatives and methods for the use thereof for the treatment of visual disorders 有权
公开(公告)号：US09388130B2
公开(公告)日：2016-07-12
申请号：US13619887
申请日：2012-09-14
申请人： Krzysztof Palczewski , Matthew Batten
发明人： Krzysztof Palczewski , Matthew Batten
IPC分类号： C07C403/06 , C07C403/12 , C07C403/14 , C07C403/10 , C07C403/20 , A61K31/22 , A61K31/215
CPC分类号： A61K31/225 , A61K9/0019 , A61K9/0048 , A61K9/0053 , A61K31/215 , A61K31/22 , C07B2200/09 , C07C403/10 , C07C403/12 , C07C403/14 , C07C403/20 , C07C2601/10 , C07C2601/16
摘要： Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided.

10. 发明申请

US20080300223A1 (20R)-2a-Methyl-19,26,27-Trinor-Vitamin D Analogs 有权
标题翻译：（20R）-2a-甲基-19,26,27-三维 - 维生素D类似物
公开(公告)号：US20080300223A1
公开(公告)日：2008-12-04
申请号：US12171085
申请日：2008-07-10
申请人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
发明人： Hector F. DeLuca , Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame
IPC分类号： A61K31/59 , C07C403/06 , A61K31/593 , A61P35/00 , A61P37/00 , A61P3/10
CPC分类号： C07C401/00
摘要： This invention discloses (20R)-2α-methyl-19,26,27-trinor-vitamin D analogs, and specifically (20R)-2α-methyl-19,26,27-trinor-1α,25-dihydroxyvitamin D3, and pharmaceutical uses therefor. This compound exhibits transcription activity as well as 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. This compound also shows very low activity in vivo on bone calcium mobilization and intestinal calcium transport activity compared to the native hormone 1α,25-dihydroxyvitamin D3, and therefore may be used to treat autoimmune disorders or inflammatory diseases in humans as well as renal osteodystrophy. This compound may also be used for the treatment or prevention of obesity.
摘要翻译：本发明公开了（20R）-2α-甲基-19,26,27-三硝基维生素D类似物，特别是（20R）-2α-甲基-19,26,27-三硝基-1α，25-二羟基维生素D 3和药物用它。该化合物显示转录活性以及阻止未分化细胞增殖并诱导其分化为单核细胞的显着活性，因此证明其用作抗癌剂并用于治疗皮肤疾病如牛皮癣以及皮肤病症如皱纹，皮肤松弛，皮肤干燥，皮脂分泌不足。与天然激素1α，25-二羟基维生素D 3相比，该化合物在体内对钙钙动员和肠钙运输活性的活性也显示出非常低的活性，因此可用于治疗人类的自身免疫性疾病或炎症性疾病以及肾性骨营养不良。该化合物也可用于治疗或预防肥胖症。

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