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    Preparation of .alpha.-tocopherol
    1.
    发明授权
    Preparation of .alpha.-tocopherol 失效
    α-生育酚的制备

    公开(公告)号：US4550182A

    公开(公告)日：1985-10-29

    申请号：US588374

    申请日：1984-03-12

    申请人： Hansgeorg Ernst ,  Henning-Peter Gehrken ,  Joachim Paust

    发明人： Hansgeorg Ernst ,  Henning-Peter Gehrken ,  Joachim Paust

    IPC分类号： C07D317/60 ,  B01J31/16 ,  C07B61/00 ,  C07D311/72

    CPC分类号： C07D311/72

    摘要： A process for the preparation of .alpha.-tocopherol of the formula I ##STR1## by reacting a chroman derivative with a C.sub.14 -Grignard reagent using a di-alkali metal tetrahalocuprate catalyst in a Schlosser-Fouquet reaction, wherein a chroman derivative of the general formula II ##STR2## where Y is a leaving group, especially Br, is used and is reacted, at from -70.degree. to 0.degree. C., first with a solution of about 1 equivalent of a Grignard compound of the general formula IIIX--Mg--R (III)where X is Cl, Br or I and R is straight-chain or branched alkyl of 1 to 14 carbon atoms, preferably methyl, ethyl or ##STR3## and then with a solution of a Grignard reagent of the formula IIIa ##STR4## in an ether solvent and a solution of a di-alkali metal tetrahalocuprate in an ether solvent. The novel process simplifies the preparation of 2RS,4'RS,8'RS-, 2R,4'RS,8'RS- or 2R,4'R,8'R-.alpha.-tocopherol by reacting a chroman structural unit, containing a C.sub.2 side-chain in the 2-position, with the corresponding C.sub.14 -Grignard compound.

    摘要翻译： 通过在Schlosser-Fouquet反应中使用二碱金属四卤代硼酸催化剂使苯并二氢吡喃衍生物与C14-格氏试剂反应制备式I的α-生育酚的方法，其中将 使用其中Y为离去基团，特别是Br的通式II（II），并且在-70℃至0℃下反应，首先用约1当量的Grignard化合物 通式III X-Mg-R（III）其中X为Cl，Br或I，R为1至14个碳原子的直链或支链烷基，优选为甲基，乙基或者“ 式IIIa的格利雅试剂（IIIa）在醚溶剂中和二碱金属四卤代硼酸酯在醚溶剂中的溶液。 该新方法简化了2RS，4'RS，8'RS-，2R，4'RS，8'RS-或2R，4'R，8'R-α-生育酚的制备，通过使色结构单元反应， 2-位的C2侧链与相应的C14-格利雅化合物。

    Novel optically active chroman derivatives, their preparation and novel intermediates
    2.
    发明授权
    Novel optically active chroman derivatives, their preparation and novel intermediates 失效
    新型光学活性苯并二氢吡喃衍生物，其制备和新型中间体

    公开(公告)号：US4645845A

    公开(公告)日：1987-02-24

    申请号：US588365

    申请日：1984-03-12

    申请人： Henning-Peter Gehrken ,  Hansgeorg Ernst ,  Joachim Paust

    发明人： Henning-Peter Gehrken ,  Hansgeorg Ernst ,  Joachim Paust

    IPC分类号： C07D311/58 ,  C07D311/72

    CPC分类号： C07D311/72

    摘要： Novel optically active chroman derivatives of the general formulae Ia and Ib ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each hydrogen or alkyl and X is --OH, --O--CO-alkyl, --O-alkyl, --O-tosyl, --O-mesyl, --O-benzenesulfonyl, Cl, Br or I, are prepared by a process in which(a) the racemate of the formula I' ##STR2## is esterified in the side chain with a carboxylic acid and then acylated with an optically active carboxylic acid halide of the general formula III ##STR3## or with the corresponding carboxylic anhydride, to give a chroman derivative IV ##STR4## or (b) the racemate I' is esterified in the side chain with the carboxylic acid from which III is derived, and, if required, the resulting ester is acylated with a carboxylic acid halide to give IV' ##STR5## the resulting mixture IV or IV', which consists of two diastereomers, is resolved by fractional crystallization, the diastereomers are hydrolyzed to the alcohols Ia and Ib and, if desired, these are converted to the other compounds Ia and Ib in a conventional manner.Useful optically active chroman derivatives Ia and Ib and diastereomeric chromanyl esters IV and IV' are also claimed.

    摘要翻译： （Ia）其中R 1，R 2，R 3和R 4各自为氢或烷基且X为-OH，-O-CO-烷基，（C 1 -C 6）烷氧基， -O-烷基，-O-甲苯磺酰基，-O-甲磺酰基，-O-苯磺酰基，Cl，Br或I是通过以下方法制备的，其中（a）式I'（I'）的外消旋物 在侧链中用羧酸酯化，然后用通式III（III）的光学活性羧酸卤化物或相应的羧酸酐进行酰化，得到苯并二氢吡喃衍生物IV（IV） 或（b）外消旋物I'在侧链中与衍生自其的羧酸酯化，如果需要，将所得酯用羧酸卤化物酰化，得到IV'（IV'） 由两个非对映异构体组成的所得混合物IV或IV'通过分级结晶来拆分，非对映异构体被水解成醇Ia和Ib，如果需要，它们是转化的 以常规方式与其它化合物Ia和Ib反应。 还要求有用的光学活性色氨酸衍生物Ia和Ib以及非对映异构的色满基酯IV和IV'。

    Preparation of canthaxanthin and astaxanthin
    6.
    发明授权
    Preparation of canthaxanthin and astaxanthin 失效
    甘氨酸和阿司匹林的制备

    公开(公告)号：US5210314A

    公开(公告)日：1993-05-11

    申请号：US695336

    申请日：1991-04-29

    申请人： Hansgeorg Ernst ,  Joachim Paust ,  Werner Hoffmann

    发明人： Hansgeorg Ernst ,  Joachim Paust ,  Werner Hoffmann

    IPC分类号： C07C45/75 ,  C07C49/653 ,  C07C49/743 ,  C07C69/63 ,  C07C403/12 ,  C07C403/24 ,  C07F9/54

    CPC分类号： C07C403/24 ,  C07C403/12 ,  C07F9/54 ,  C07F9/5435 ,  C07C2101/16

    摘要： A process for preparing canthaxanthin (Ia) and astaxanthin (Ib) of the formula I ##STR1##where R is H (a) or OH (b), comprises reacting a tertiary alcohol of the formula II ##STR2##where R is H (a) or OH (b), with trifluoroacetic acid, reacting the resulting novel trifluoroacetate of the formula III ##STR3##with triphenylphosphine, and reacting the resulting novel triphenylphosphonium trifluoroacetate of the formula IV ##STR4## with 2,7-dimethyl-2,4,6-octatriene-1,8-dial under the conditions of a Wittig synthesis. The present invention also relates to the novel trifluoroacetates of the formula III and the corresponding triphenylphosphonium trifluoroacetates of the formula IV.

    摘要翻译： 制备式I的角黄素（Ia）和虾青素（Ib）的方法，其中R是H（a）或OH（b））包括使式II的叔醇（II）与R （III）的三氟乙酸盐与三苯基膦反应，并使得到的式IV的三氟化三苯基鏻（Ⅳ）与式（Ⅳ）化合物反应，得到新的三氟乙酸盐， 在Wittig合成条件下用2,7-二甲基-2,4,6-辛二烯-1,8-表盘。 本发明还涉及式III的新型三氟乙酸盐和式Ⅳ相应的三苯基三氟乙酸盐。

    Preparation of 2-n-propyl-4-amino-5-methoxymethyl-pyrimidine
    7.
    发明授权
    Preparation of 2-n-propyl-4-amino-5-methoxymethyl-pyrimidine 失效
    2-正丙基-4-氨基-5-甲氧基甲基 - 嘧啶的制备

    公开(公告)号：US4918191A

    公开(公告)日：1990-04-17

    申请号：US393976

    申请日：1989-08-15

    申请人： Joachim Paust ,  Hansgeorg Ernst

    发明人： Joachim Paust ,  Hansgeorg Ernst

    IPC分类号： C07D239/42

    CPC分类号： C07D239/42

    摘要： In an improved process for the preparation of 2-n-propyl-4-amino-5-methoxymethyl-pyrimidine of the formula I ##STR1## by reacting butyramidine II ##STR2## with .alpha.-methoxymethyl-.beta.-methoxyacrylonitrile III ##STR3## the butyramidine II is reacted with a 0.4-5 molar excess of .alpha.-methoxymethyl-.beta.-methoxyacrylonitrile III at from -10.degree. to +20.degree. C.

    摘要翻译： 通过使丁酰脒II II与α​​-甲氧基甲基-β-甲氧基丙烯腈III反应制备式I的2-正丙基-4-氨基-5-甲氧基甲基 - 嘧啶的改进方法III IMA图 > III，在-10℃至+ 20℃下，使丁酰脒II与0.4-5摩尔过量的α-甲氧基甲基-β-甲氧基丙烯腈III反应。

    Epimerization of sugars, in particular of D-arabinose to D-ribose
    8.
    发明授权
    Epimerization of sugars, in particular of D-arabinose to D-ribose 失效
    糖异构化，特别是D-阿拉伯糖对D-核糖

    公开(公告)号：US4778531A

    公开(公告)日：1988-10-18

    申请号：US68171

    申请日：1987-06-30

    申请人： Walter Dobler ,  Hansgeorg Ernst ,  Joachim Paust

    发明人： Walter Dobler ,  Hansgeorg Ernst ,  Joachim Paust

    IPC分类号： C07B61/00 ,  C07H3/00 ,  C07H3/02 ,  C07H1/00 ,  C13J1/06

    CPC分类号： C07H3/02

    摘要： Pentoses and hexoses are epimerized by heating sugar dissolved in a solvent in the presence of a molybdenum(VI) compound, by an improved process in which, for the preparation of a sugar having cis OH groups in the 2- or 3-position, of the formula Ia or Ib ##STR1## where R is one of the radicals ##STR2## a homogeneous solution of the corresponding sugar of the formula IIa or IIb ##STR3## is heated to 75.degree.-100.degree. C. in the presence of from 30 to 200 mol %, based on sugar used, of a metal salt of the formula (III)MeX.sub.2 (III)where Me is Mg, Ca, Sr, Ba or Zn and X is Cl or Br, which may or may not contain water of crystallization, and in the presence of from 2 to 20 mol %, based on the sugar used, of a molybdenum(VI) compound.The process is particularly important for the preparation of D-ribose, which is required as an intermediate for vitamin B.sub.2.

    摘要翻译： 戊糖和己糖通过加热溶解在钼（VI）化合物存在下的溶剂中的糖进行差向异构化，其中通过改进方法，其中为了制备在2-或3-位具有顺式OH基团的糖， 式Ia或Ib的化合物，其中R是式IIa或IIb的相应糖的均匀溶液之一的基团之一，在30℃的存在下加热至75℃-100℃ （III）的MeX2（III）的金属盐，其中Me是Mg，Ca，Sr，Ba或Zn，X是Cl或Br，其可以含有或可以不含水 的结晶，并且在基于所用糖的2至20摩尔％的存在下，使用钼（VI）化合物。 该方法对于制备作为维生素B2的中间体的D-核糖是特别重要的。

    Preparation of riboflavin
    9.
    发明授权
    Preparation of riboflavin 失效
    核黄素的制备

    公开(公告)号：US4567261A

    公开(公告)日：1986-01-28

    申请号：US570457

    申请日：1984-01-13

    申请人： Hansgeorg Ernst ,  Wolfram Schmidt ,  Joachim Paust

    发明人： Hansgeorg Ernst ,  Wolfram Schmidt ,  Joachim Paust

    IPC分类号： C07D475/14 ,  C07D475/02

    CPC分类号： C07D475/02

    摘要： Riboflavin of the formula I ##STR1## is prepared by condensing a 4,5-dimethyl-N-(D)-ribityl-2-phenylazoaniline of the formula II ##STR2## where R is H or --Cl, --NO.sub.2 or --CH.sub.3 in the o- or p-position, with barbituric acid of the formula III ##STR3## in the presence of an acid as the condensing agent, by an improved process in which the acidic condensing agent used is an aliphatic or cycloaliphatic/aliphatic tertiary carboxylic acid of the general formula IV ##STR4## where R.sup.1, R.sup.2 and R.sup.3 are each a lower alkyl group, R.sup.1, R.sup.2 and R.sup.3 together containing 3 to 20, preferably 3 to 10, carbon atoms, or R.sup.1 is a lower alkyl group, in particular methyl, and R.sup.2 and R.sup.3 together form a tetramethylene or pentamethylene group.The process can be particularly advantageously carried out using trimethylacetic acid or a commercial mixture of saturated tertiary carboxylic acids, e.g. Versatic .sup.R 10-acid.

    摘要翻译： 式I（I）的核黄素通过将式II的4,5-二甲基-N-（D） - 二乙基苯基偶氮苯胺（II）缩合制备，其中R是H或-Cl ，在邻位或对位的-NO 2或-CH 3与通式III的巴比妥酸（III）在作为缩合剂的酸存在下，通过改进的方法，其中使用酸性缩合剂 是通式IV（IV）的脂族或脂环族/脂肪族三羧酸，其中R 1，R 2和R 3各自为低级烷基，R 1，R 2和R 3一起含有3至20，优选3至10， 碳原子，或R 1是低级烷基，特别是甲基，R 2和R 3一起形成四亚甲基或五亚甲基。 该方法可以特别有利地使用三甲基乙酸或饱和叔羧酸的商业混合物，例如， 通用R10酸。

    Preparation of N-acylamino acid esters and N-acylamino acetals
    10.
    发明授权
    Preparation of N-acylamino acid esters and N-acylamino acetals 失效
    N-酰基氨基酸酯和N-酰基氨基缩醛的制备

    公开(公告)号：US06740774B1

    公开(公告)日：2004-05-25

    申请号：US09639681

    申请日：2000-08-16

    申请人： Joachim Paust ,  Hansgeorg Ernst ,  Reinhard Kaczmarek ,  Hagen Jaedicke

    发明人： Joachim Paust ,  Hansgeorg Ernst ,  Reinhard Kaczmarek ,  Hagen Jaedicke

    IPC分类号： C07C22900

    CPC分类号： C07C231/08 ,  C07C233/18 ,  C07C233/47

    摘要： A process for preparing N-acyl derivatives of the formula I, in which the substituents independently of one another have the following meanings: X is CH(OR3)2, COOR3; R1 is hydrogen, C1-C12-alkyl, aryl, unsubstituted or substituted; R2 is hydrogen, C1-C12-alkyl, aryl, unsubstituted or substituted; R3 is C1-C12-alkyl, which comprises reacting a carboxamide R1—CONH2 of the formula II with a glyoxal monoacetal derivative of the formula III, in the presence of a carboxylic acid R4—COOH of the formula IV where R4=C1-C12-alkyl, where the substituents R1 to R3 are as defined above, is described.

    摘要翻译： 制备式I的N-酰基衍生物的方法，其中取代基彼此独立地具有以下含义：X是CH（OR 3）2，COOR 3; R 1是氢，C 1 C 12 - 烷基，芳基，未取代或取代的; R 2是氢，C 1 -C 12 - 烷基，芳基，未取代或取代的; R 3是C 1 -C 12烷基，其包括使羧酰胺R 1， -CONH 2与式III的乙二醛单缩醛衍生物在式IV的羧酸R 4 -COOH的存在下反应，其中R 4 = C 1 -C 12 - 烷基，其中取代基R' 1> -R 3如上所定义。