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81. 发明授权

US4725689A Preparation of 2-amino-3-cyano-5-dialkoxymethylpyrazines and intermediates for this method 失效
标题翻译： 2-氨基-3-氰基-5-二烷氧基甲基吡嗪的制备及其制备方法
公开(公告)号：US4725689A
公开(公告)日：1988-02-16
申请号：US776462
申请日：1985-09-16
申请人： Hartmut Leininger , Wolfgang Littmann , Joachim Paust
发明人： Hartmut Leininger , Wolfgang Littmann , Joachim Paust
IPC分类号： C07D241/20 , C07D241/26 , C07D403/04 , C07D475/04
CPC分类号： C07D403/04 , C07D241/20 , C07D241/26 , Y02P20/55
摘要： 2-Amino-3-cyano-5-dialkoxymethylpyrazine derivatives of the general formula III ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or a protective group usually employed for amino groups and R.sup.5 and R.sup.6 are each alkyl of 1 to 4 carbon atoms, or together form an ethylene or propylene radical which is unsubstituted or substituted by methyl, are prepared starting from a novel 3-halomethyl-5-dihalomethyl-2-aminopyrazine derivative of the formula IV ##STR2## where X is Cl or Br, via a novel intermediate of the general formula I ##STR3## where R.sup.3 is --CH.sub.2 --O--CO--CH.sub.3 (a), --CH.sub.2 OH (b), ##STR4## or --C.tbd.N (d) and R.sup.4 is --CHCl.sub.2 or --CHBr.sub.2 or, where R.sup.1 and R.sup.2 are each a protective group, R.sup.4 may furthermore be ##STR5##The compounds according to the invention are useful intermediates for the preparation of folic acid and active compounds derived from this.
摘要翻译：通式III（III）的2-氨基-3-氰基-5-二烷氧基甲基吡嗪衍生物其中R 1和R 2各自为氢或通常用于氨基的保护基，R 5和R 6各自为1-4的烷基碳原子，或一起形成未被取代或被甲基取代的乙烯或丙烯基团，由式IV（IV）的新型3-卤代甲基-5-二卤代甲基-2-氨基吡嗪衍生物制备，其中X为 Cl或Br通过通式I的新型中间体（I），其中R 3是-CH 2 -O-CO-CH 3（a），-CH 2 OH（b），（c）或-C 3 N（d）和R4是-CHCl 2或-CHBr 2，或者其中R 1和R 2各自是保护基，R 4还可以是本发明的化合物是用于制备叶酸和活性化合物的有用中间体由此。

82. 发明授权

US4716243A .alpha.-(o-chlorophenyl)-aminomethylene-.beta.-formylaminopropionitrile 失效
标题翻译： α-（邻氯苯基） - 氨基亚甲基-β-甲酰基氨基丙腈
公开(公告)号：US4716243A
公开(公告)日：1987-12-29
申请号：US765505
申请日：1985-08-15
申请人： Hansgeorg Ernst , Wolfgang Littmann , Joachim Paust
发明人： Hansgeorg Ernst , Wolfgang Littmann , Joachim Paust
IPC分类号： C07C67/00 , C07C253/00 , C07C253/30 , C07C255/27 , C07C255/30 , C07D239/42 , C07C87/24 , C07C121/16
CPC分类号： C07D239/42 , C07C255/00
摘要： .alpha.-(o-Chlorophenyl)-aminomethylene-.beta.-formylaminopropionitrile, process for its preparation by reacting a metal salt of .alpha.-formyl-.beta.-formylaminopropionitrile with a salt of o-chloroaniline in an aqueous medium, and use of the product to prepare the compound of the formula ##STR1## by reaction with acetamidine. The pyrimidine thus obtained is an intermediate for the preparation of vitamin B.sub.1.
摘要翻译： α-（甲基 - 氯苯基） - 氨基亚甲基-β-甲酰基氨基丙腈的制备方法，其通过使α-甲酰基-β-甲酰氨基丙腈的金属盐与邻氯苯胺的盐在水性介质中反应制备，通过与乙脒反应制备式“IMAGE”的化合物。由此获得的嘧啶是制备维生素B1的中间体。

83. 发明授权

US4681936A Preparation of sugar ketals 失效
标题翻译：糖缩酮的制备
公开(公告)号：US4681936A
公开(公告)日：1987-07-21
申请号：US826317
申请日：1986-02-05
申请人： Klaus-Peter Pfaff , Joachim Paust , Horst Hartmann
发明人： Klaus-Peter Pfaff , Joachim Paust , Horst Hartmann
IPC分类号： C07H1/00 , B01J31/00 , C07B61/00 , C07H9/04
CPC分类号： C07H9/04
摘要： Sugar ketals are prepared by reacting a sugar with a ketone in the presence of an acid catalyst by a process in whichA. a molecular boron trifluoride compound or trifluoromethanesulfonic acid is used in an amount of only from 0.01 to 10% by weight, based on the sugar used,B. up to a 30-fold molar excess of the ketone is used andC. the water formed during the reaction is removed continuously from the reaction mixture.In a particularly advantageous embodiment of the process, the boron trifluoride is used in the form of boron trifluoride etherate and, when the reaction is complete, this compound or the trifluoromethanesulfonic acid is rendered ineffective under non-aqueous conditions, after which the ketone is evaporated off and the reaction mixture is then subjected to fractional distillation. The process is particularly important for the reaction of L-sorbose with acetone to obtain 2,3:4,6-di-O-isopropylidene-L-sorbofuranose, which is required for the synthesis of ascorbic acid.
摘要翻译：糖缩成物是通过在酸催化剂存在下使糖与酮反应的方法制备的，其中A为分子三氟化硼化合物或三氟甲磺酸的用量，其量仅为0.01至10重量％，基于使用的糖，B.使用高达30倍摩尔过量的酮，并且C.从反应混合物中连续除去反应期间形成的水。在该方法的特别有利的实施方案中，三氟化硼以三氟化硼醚合物的形式使用，当反应完成时，该化合物或三氟甲磺酸在非水性条件下变得无效，之后酮蒸发然后将反应混合物进行分馏。该方法对于L-山梨糖与丙酮的反应特别重要，得到合成抗坏血酸所需的2,3：4,6-二-O-异亚丙基-L-山梨糖。

84. 发明授权

US4656275A Preparation of riboflavin, and 4,5-dimethyl-N-(D)-ribityl-2-(O-alkoxyphenylazo)-aniline intermediates 失效
标题翻译：制备核黄素和4,5-二甲基-N-（D） - 二丙基-2-（O-烷氧基苯偶氮） - 苯胺中间体
公开(公告)号：US4656275A
公开(公告)日：1987-04-07
申请号：US730056
申请日：1985-05-03
申请人： Hansgeorg Ernst , Heinz Eckhardt , Joachim Paust
发明人： Hansgeorg Ernst , Heinz Eckhardt , Joachim Paust
IPC分类号： C07C67/00 , C07C241/00 , C07C245/08 , C07D475/14 , C07C107/06
CPC分类号： C07D475/14
摘要： An improved process for the preparation of riboflavin by condensation of a 4,5-dimethyl-N-(D)-ribityl-2-phenylazoaniline derivative with barbituric acid in the presence of an acidic condensing agent in an organic solvent, wherein a 4,5-dimethyl-N-(D)-ribityl-2-(o-alkoxyphenylazo)-aniline of the formula IIa ##STR1## where R is alkyl of 1 to 4 carbon atoms, in particular methyl, is reacted with barbituric acid, as well as the novel intermediates of the formula IIa.
摘要翻译：一种改进的制备核黄素的方法，其通过在酸性缩合剂存在下，在有机溶剂中使4,5-二甲基-N-（D） - 间苯基] -2-苯基偶氮苯胺衍生物与巴比妥酸缩合，其中R是1至4个碳原子的烷基，特别是甲基的式IIa的（R） - （2-（O-）烷基-2-（邻 - 烷氧基苯基偶氮） - 苯胺其中R是与巴比妥酸反应，以及式IIa的新型中间体。

85. 发明授权

US4645845A Novel optically active chroman derivatives, their preparation and novel intermediates 失效
标题翻译：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'。

86. 发明授权

US4360669A Preparation of N-(D)-ribityl-2-phenylazo-4,5-dimethylaniline 失效
标题翻译： N-（D） - 基] -2-苯基偶氮-4,5-二甲基苯胺的制备
公开(公告)号：US4360669A
公开(公告)日：1982-11-23
申请号：US286601
申请日：1981-07-24
申请人： Wolfram Schmidt , Joachim Paust , Axel Nurrenbach
发明人： Wolfram Schmidt , Joachim Paust , Axel Nurrenbach
IPC分类号： C07C67/00 , C07C215/10 , C07C241/00 , C07C245/08 , C07D475/14 , C07H1/00 , C07H1/06
CPC分类号： C07D475/14
摘要： A process for the preparation of N-(D)-ribityl-2-phenylazo-4,5-dimethylaniline (I), wherein1. in the case of pure or virtually pure (D)-ribose (III)(a) the latter is reacted with 3,4-dimethylnitrobenzene (IVa) or 3,4-dimethylaniline (IVb) and with hydrogen in the presence of a hydrogenation catalyst,(b) the resulting solution is reacted, in a conventional manner, with an acid phenyldiazonium salt solution (VI) and(c) the resulting product is isolated by crystallization, in a conventional manner, or2. in the case of crude ribose, ie. industrial mixtures of (D)-ribose and other sugars(a) the crude ribose is reacted with about equimolar amounts, based on III, of 3,4-dimethylaniline (IVb) and boric acid,(b) the boric acid ester of the Schiff base obtained from III and IVb is allowed to crystallize out and is separated off,(c) this ester is hydrogenated with hydrogen in the presence of a hydrogenation catalyst,(d) the solution is freed from catalyst and reacted, in a conventional manner, with an acid phenyldiazonium salt solution and(e) the resulting product I is isolated by crystallization in a conventional manner.
摘要翻译：制备N-（D） - 基] -2-苯基偶氮基-4,5-二甲基苯胺（I）的方法，其中1.在纯的或几乎纯的（D） - 核糖（III）（a）的情况下，后者与3,4-二甲基硝基苯（IVa）或3,4-二甲基苯胺（IVb）和氢气在氢化催化剂存在下反应，（b）所得溶液以常规方式与酸性苯基重氮盐溶液（VI）和（c）通过以常规方式结晶分离得到的产物，或在粗核糖的情况下，（D） - 核糖和其他糖（a）的工业混合物（a）粗核糖基于III，3,4-二甲基苯胺（IVb）和硼酸，以（b）硼酸酯的大约等摩尔量反应允许从III和IVb获得的席夫碱结晶出并分离出来，（c）在氢化催化剂存在下，用氢气氢化该酯，（d）将溶液除去催化剂并以常规方式反应用酸性苯基重氮盐溶液和（e）所得到的产物I通过常规方式结晶分离。

87. 发明授权

US4212827A Manufacture of canthaxanthin 失效
标题翻译：角黄素的制造
公开(公告)号：US4212827A
公开(公告)日：1980-07-15
申请号：US841697
申请日：1977-10-13
申请人： Joachim Paust , Joachim Schneider , Hagen Jaedicke
发明人： Joachim Paust , Joachim Schneider , Hagen Jaedicke
IPC分类号： C07B61/00 , B01J21/00 , B01J23/00 , C07C20060101 , C07C49/21 , C07C49/653 , C07C67/00 , C07C67/30 , C07C69/52 , C07C401/00 , C07C403/00 , C07C403/24 , C07C45/02
CPC分类号： C07C403/24
摘要： Process for the manufacture of canthaxanthin by oxidizing .beta.-carotene, retro-dehydro-carotene or echinenone with a salt of chloric or bromic acid in the presence of a catalyst and of an inert diluent or solvent.
摘要翻译：通过在催化剂和惰性稀释剂或溶剂的存在下，用氯或溴酸的盐氧化β-胡萝卜素，逆 - 脱氢胡萝卜素或氢化chin酮来制造角黄素的方法。

88. 发明授权

US4044026A Substituted succinaldehyde monoacetals 失效
标题翻译：取代的琥珀醛单缩醛
公开(公告)号：US4044026A
公开(公告)日：1977-08-23
申请号：US523442
申请日：1974-11-13
申请人： Joachim Paust
发明人： Joachim Paust
IPC分类号： A01N35/02 , C07C45/00 , C07C45/64 , C07C45/70 , C07C45/71 , C07C47/198 , C07C47/24 , C07C47/277 , C07C67/00 , C07D317/26 , C07C47/02
CPC分类号： C07C47/198 , C07C45/70 , C07C45/71 , C07C47/277 , C07D317/26
摘要： New substituted succinaldehyde monoacetals which are produced by introducing an .alpha., .beta.-unsaturated aldehyde bearing halogen, arylsulfonyl or alkylsulfonyl as a substituent in the .gamma.-position into a solution of an alkali metal alcoholate, an alkali metal glycolate or an alkali metal phenolate in a lower alcohol at a temperature of less than 50.degree. C. The new succinaldehyde monoacetals are of great interest as intermediates in the production of perfumes and of terpene derivatives of the type of juvenile hormones.
摘要翻译：新的取代的琥珀醛单缩醛，其通过将含有卤素，芳基磺酰基或烷基磺酰基的α，β-不饱和醛作为γ-位点中的取代基引入到碱金属醇盐，碱金属乙醇酸盐或碱金属酚盐的溶液中而制备低于50℃的低级醇。新型琥珀醛单缩醛作为生产香料和少ile激素类型的萜烯衍生物的中间体是非常有意义的。

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