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1. 发明申请

WO2009016025A1 PROCESS FOR THE SYNTHESIS OF NA- BETA-ALANINATE AND CALCIUM PANTOTHENATE 审中-公开
标题翻译：合成NA-BETA-ALANINATE和CALCUM PANTOTHENATE的方法
公开(公告)号：WO2009016025A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059201
申请日：2008-07-15
申请人： DSM IP ASSETS B.V. , EISELE, Frank , KARGE, Reinhard , SPRUIJTENBURG, Robert
发明人： EISELE, Frank , KARGE, Reinhard , SPRUIJTENBURG, Robert
IPC分类号： C07C229/08 , C07C227/02 , C07C231/02 , C07C235/12 , C07C227/38
CPC分类号： C07C227/26 , C07C229/08 , C07C231/10 , C07C235/12
摘要： In a process for the preparation of Na-β-alaninate from β-amino-propionitrile ready for the condensation with pantolactone to pantothenate the improvement of obtaining Na-β-alaninate as a solution in an alcohol, which improvement comprises carrying out the hydrolysis of β-amino-propionitrile in water and then making a solvent exchange from water to an alcohol, thus achieving that the final β-alaninate mixture contains side- or by-products in amounts only, which do not negatively influence the-pantothenate quality.
摘要翻译：在用于与泛酸内酯缩合的β-氨基丙腈制备Na-β-丙氨酸酯的方法中，可以提高获得作为醇溶液的Na-β-丙氨酸酯的改进，该改进包括进行水解 β-氨基 - 丙腈在水中，然后从水中进行溶剂交换至醇，从而实现最终的β-丙氨酸酯混合物仅含有副产物或副产物，其不会对泛酸盐质量产生不利影响。

2. 发明申请

WO2010115950A3 PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES 审中-公开
公开(公告)号：WO2010115950A3
公开(公告)日：2010-10-14
申请号：PCT/EP2010/054629
申请日：2010-04-08
申请人： DSM IP ASSETS B.V. , SCHÜTZ, Jan , KARGE, Reinhard
发明人： SCHÜTZ, Jan , KARGE, Reinhard
IPC分类号： C07D239/42
摘要： A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula (I) wherein R is CONH 2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H 2 N CH = C(R) CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula (I) is transferred into an acid addition salt, and the transformation of a compound of formula (Il) wherein R is CONH 2 into a compound of formula (Il) wherein R is CN by treatment with POCI 3 .

3. 发明申请

WO2011131607A1 ISOMERIZATION OF β-KETO-ALLENES 审中-公开
标题翻译： ß-KETO-ALLENES的异构体
公开(公告)号：WO2011131607A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056106
申请日：2011-04-18
申请人： DSM IP ASSETS B.V. , BONRATH, Werner , KARGE, Reinhard , NETSCHER, Thomas
发明人： BONRATH, Werner , KARGE, Reinhard , NETSCHER, Thomas
IPC分类号： C07C49/203
CPC分类号： C07C45/67 , B01J31/08 , B01J2231/52 , C07C49/203
摘要： Isomerization of β-keto-allenes of the general formula I wherein R 1 is hydrogen, methyl or ethyl, in particular hydrogen or methyl; R 2 is hydrogen or methyl; R 3 is hydrogen or methyl, in particular methyl and R 4 is an aliphatic hydrocarbon residue containing 1 - 37 carbon atoms, into corresponding α,γ-dienones of formula II by treatment with a basic ion exchange resin.
摘要翻译：其中R 1是氢，甲基或乙基，特别是氢或甲基的通式I的β-酮 - 双烯异构化; R2是氢或甲基; R 3是氢或甲基，特别是甲基，R 4是含有1至37个碳原子的脂族烃残基，通过用碱性离子交换树脂处理而形成相应的式II的α-二烯酮。

4. 发明申请

WO2010079123A2 PROCESS FOR RESVERATROL INTERMEDIATE 审中-公开
标题翻译： RESVERATROL INTERMEDIATE过程
公开(公告)号：WO2010079123A2
公开(公告)日：2010-07-15
申请号：PCT/EP2010/000021
申请日：2010-01-06
申请人： DSM IP ASSETS B.V. , BONRATH, Werner , LETINOIS, Ulla , HUGENTOBLER, Max , KARGE, Reinhard , LEHMANN, Hajo
发明人： BONRATH, Werner , LETINOIS, Ulla , HUGENTOBLER, Max , KARGE, Reinhard , LEHMANN, Hajo
IPC分类号： C07C39/215 , C07C69/017 , C07C67/28
CPC分类号： C07C67/29 , C07C69/017 , C07C69/18
摘要： A process for the preparation of 1-(3,5-diacetoxyphenyl)-ethanol by catalytic hydrogenation of 3,5-diacetoxy-acetophenone in the presence of a Ni-alloy as catalyst in a C 1-3 -carboxylic acid ester as solvent.
摘要翻译：在作为溶剂的C 3-羧酸酯中的Ni合金作为催化剂存在下，通过3,5-二乙酰氧基 - 苯乙酮的催化氢化制备1-（3,5-二乙酰氧基苯基） - 乙醇的方法。

5. 发明申请

WO2010010113A1 Novel synthesis of substituted 4-amino-pyrimidines 审中-公开
标题翻译：取代的4-氨基 - 嘧啶的新型合成
公开(公告)号：WO2010010113A1
公开(公告)日：2010-01-28
申请号：PCT/EP2009/059415
申请日：2009-07-22
申请人： DSM IP ASSETS B.V. , KARGE, Reinhard , LETINOIS, Ulla , SCHIEFER, Gerhard
发明人： KARGE, Reinhard , LETINOIS, Ulla , SCHIEFER, Gerhard
IPC分类号： C07C255/30 , C07C271/20
CPC分类号： C07C255/30 , C07C271/20 , Y02P20/55
摘要： The present invention is directed to a process for the manufacture of compounds of formula IV wherein R 1 is an amino protecting group, and R 2 is hydrogen or C 1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M + is a cation, preferably selected from the group consisting of Li + , Na+, K + , 1/2 Mg 2+ and 1/2 Zn 2+ , (formula 1a) with an ammonium salt NH 4 + X - , wherein X - is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R 2 -CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B 1 .
摘要翻译：本发明涉及制备式IV化合物的方法，其中R 1是氨基保护基，R 2是氢或C 1-10烷基，其包括a）使式Ia化合物（其中M +是阳离子）优选选自Li +，Na +，K +，1/2 Mg2 +和1/2 Zn2 +，（式1a）与铵盐NH4 + X-，其中X是阴离子，优选选自氯化物，溴化物，硫酸盐和乙酸盐，在溶剂中加入式II的化合物中。b）使碱式化合物与碱的存在下的腈R2-CN反应，得到式Ⅳ化合物。本发明还涉及式II化合物及其制备维生素B1的用途。

6. 发明申请

WO2004087640A1 PROCESS FOR THE MANUFACTURE OF N-ALKOXALYL-ALANINATES 审中-公开
标题翻译：制备N-烷氧基 - 兰酸酯的方法
公开(公告)号：WO2004087640A1
公开(公告)日：2004-10-14
申请号：PCT/EP2004/003109
申请日：2004-03-24
申请人： DSM IP ASSETS B.V. , GUM, Andrew, George , FISCHESSER, Jocelyn , HÄRTER, Ralph , KARGE, Reinhard , JEPHCOTE, Vincent, John , BONRATH, Werner
发明人： GUM, Andrew, George , FISCHESSER, Jocelyn , HÄRTER, Ralph , KARGE, Reinhard , JEPHCOTE, Vincent, John , BONRATH, Werner
IPC分类号： C07C233/47
CPC分类号： C07C233/47 , C07C231/02
摘要： A process for the manufacture of alkyl N-alkoxalyl-alaninates of the formula alkylO-CO-CO-NH-CH(CH 3 )-CO-Oalkyl comprises reacting alanine with a dialkyl oxalate under substantially non-acidic conditions, which may be created by carrying out the reaction in the presence of a base. The reaction may furthermore be carried out in the presence of added alkanol, preferably one featuring the alkyl group corresponding to that of the employed dialkyl oxalate. The monoesters N-alkoxalyl-alanine of the formula alkylO-CO-CO-NH-CH(CH 3 )-COOH, which as intermediates in the process can be isolated therefrom, are novel and as such are also an object of the present invention. The alkyl N-alkoxalylalaninates are useful intermediates in the multistep process for the manufacture of vitamin B 6 .
摘要翻译：制备式为烷基O-CO-CO-NH-CH（CH 3）-CO-O烷基的N-烷氧基甲硅烷基烷基酯的方法包括在基本上非酸性条件下使丙氨酸与草酸二烷基酯反应，其可以由在碱的存在下进行反应。此外，反应可以在添加的链烷醇的存在下进行，优选的是具有对应于所使用的草酸二烷基酯的烷基的烷基。作为本方法中的中间体的式为烷基O-CO-CO-NH-CH（CH 3）-COOH的单酯N-烷氧基 - 丙氨酸是新颖的，因此也是本发明的目的。 N-烷氧基烷基丙氨酸烷基酯是制造维生素B6的多步法中有用的中间体。

7. 发明申请

WO2013010811A1 PROCESS FOR THE OXIDATION OF SORBOSE 审中-公开
标题翻译： SORBOSE氧化工艺
公开(公告)号：WO2013010811A1
公开(公告)日：2013-01-24
申请号：PCT/EP2012/063205
申请日：2012-07-06
申请人： DSM IP Assets B.V. , BONRATH, Werner , GRÜNEWALD, Elena , KARGE, Reinhard , MEDLOCK, Jonathan , PRÜSSE, Ulf , VORLOP, Klaus
发明人： BONRATH, Werner , GRÜNEWALD, Elena , KARGE, Reinhard , MEDLOCK, Jonathan , PRÜSSE, Ulf , VORLOP, Klaus
IPC分类号： B01J23/52 , C07C51/235 , C07C59/215
CPC分类号： C07H1/00 , B01J23/52 , C07C51/235 , C07H3/02 , C07H7/027 , C07C59/215
摘要： The present invention relates to a process for the oxidation of sorbose using a specific catalyst, as well as to the catalyst as such.
摘要翻译：本发明涉及使用特定催化剂以及催化剂氧化山梨糖的方法。

8. 发明申请

WO2006108636A1 MANUFACTURE OF THIOLACTONES 审中-公开
标题翻译：制造THIOLACTONES
公开(公告)号：WO2006108636A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003375
申请日：2006-04-12
申请人： DSM IP ASSETS B.V. , BONRATH, Werner , KARGE, Reinhard , ROESSLER, Felix
发明人： BONRATH, Werner , KARGE, Reinhard , ROESSLER, Felix
IPC分类号： B01J23/46 , C07D495/04
CPC分类号： B01J31/24 , B01J23/468 , B01J2531/827 , C07D495/04
摘要： The present invention relates to a process for the manufacture of cyclic thio esters (thiolactones) and related compounds by hydrogenation of cyclic thioanhydrides in the presence of metal catalysts.
摘要翻译：本发明涉及在金属催化剂存在下通过氢化环硫代氢化物制备环硫代酯（硫代内酯）和相关化合物的方法。

9. 发明申请

WO2006108562A1 MANUFACTURE OF LACTONES 审中-公开
标题翻译：制品的制造
公开(公告)号：WO2006108562A1
公开(公告)日：2006-10-19
申请号：PCT/EP2006/003163
申请日：2006-04-07
申请人： DSM IP ASSETS B.V. , BONRATH, Werner , KARGE, Reinhard , ROESSLER, Felix
发明人： BONRATH, Werner , KARGE, Reinhard , ROESSLER, Felix
IPC分类号： B01J23/46 , C07D491/04
CPC分类号： C07D491/04 , B01J31/24 , B01J2531/822
摘要： The present invention relates to a process for the manufacture of cyclic monocarboxylic esters (lactones) and related compounds by hydrogenation of cyclic dicarboxylic acid anhydrides in the presence of metal catalysts.
摘要翻译：本发明涉及在金属催化剂存在下通过环状二羧酸酐的氢化制备环状单羧酸酯（内酯）和相关化合物的方法。

10. 发明申请

WO2005049618A1 MANUFACTURE OF VITAMIN B6 审中-公开
标题翻译：维生素B6的制备
公开(公告)号：WO2005049618A1
公开(公告)日：2005-06-02
申请号：PCT/EP2004/012655
申请日：2004-11-09
申请人： DSM IP ASSETS B.V. , FISCHESSER, Jocelyn , FRITSCH, Helmut , GUM, Andrew, George , KARGE, Reinhard , KEUPER, Ralf
发明人： FISCHESSER, Jocelyn , FRITSCH, Helmut , GUM, Andrew, George , KARGE, Reinhard , KEUPER, Ralf
IPC分类号： C07D491/04
CPC分类号： C07D491/04 , Y02P20/582
摘要： A process for manufacturing a 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 9-acyloxy-1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin (I) and optionally for manufacturing pyridoxine involves performing an addition reaction between a 4-methyl-5-alkoxy-oxazole (II) and a 2-unsubstituted, 2-monosubstituted or 2,2-disubstituted 4,7-dihydro-(1,3)-dioxepin (III) in the substantial absence of a solvent and a catalyst to give a product mixture consisting essentially of the appropriate Diels-Alder adduct (IV) in a major proportion and the appropriate 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin 9-ol (V) in a minor proportion, removal of a substantial proportion of the unreacted oxazole and dioxapin starting materials from the product mixture by distillation under reduced pressure, addition of a substantially anhydrous organic acid to said product mixture and rearrangement of the Diels-Alder adduct IV to further V in the presence of said substantially anhydrous organic acid with removal of the generated alkanol by distillation under reduced pressure, and acylation of the resultingly enriched quantity of V with an added carboxylic acid anhydride to produce the desired I, and optionally converting this so-manufactured acylation product I to pyridoxine by acid hydrolysis for achieving deprotection and deacylatiom. Pyridoxine is a well known form of vitamin B 6 with well established utility.
摘要翻译：制备3-未取代的3-单取代的或3,3-二取代的9-酰氧基-1,5-二氢-8-甲基吡啶并[3,4-e] [1,3]二氧杂环庚烯（I）的方法，制备吡哆醛涉及在4-甲基-5-烷氧基 - 恶唑（II）和2-未取代的2-单取代或2,2-二取代的4,7-二氢 - （1,3）二氧杂环己烷 III）在基本上不存在溶剂和催化剂的情况下得到基本上由主要比例的合适的狄尔斯 - 阿尔德加合物（IV）组成的产物混合物和合适的3-未取代的3-单取代的或3,3-二取代的1 ，5-二氢-8-甲基吡啶并[3,4-e] [1,3]二氧杂环庚烷-9-醇（V），少量比例地从产物混合物中除去大部分未反应的恶唑和二氧杂环己烯起始原料在减压下蒸馏，向所述产物混合物中加入基本上无水的有机酸，并且将狄尔斯 - 阿尔德加合物IV重新排列成pr 通过减压蒸馏除去生成的链烷醇，然后用加入的羧酸酐酰化所得的富集量的V，从而产生所需的I，并且任选地将这样制得的酰化产物I 通过酸水解获得吡哆醛，以实现去保护和脱酰基。吡哆素是众所周知的维生素B6形式，具有很好的实用性。

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