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1. 发明授权

US5811588A Process for the preparation of 3-phenylpropanal 失效
标题翻译： 3-苯基丙醛的制备方法
公开(公告)号：US5811588A
公开(公告)日：1998-09-22
申请号：US834456
申请日：1997-04-16
申请人： Anna M. C. F. Castelijns , Johanna M. Hogeweg , Simon P. J. M. van Nispen
发明人： Anna M. C. F. Castelijns , Johanna M. Hogeweg , Simon P. J. M. van Nispen
IPC分类号： C07B61/00 , C07C45/62 , C07C47/228 , C07C51/235 , C07C51/255 , C07C57/30
CPC分类号： C07C45/62 , C07C51/235
摘要： Process for the preparation of 3-phenylpropanal in which cinnamaldehyde is hydrogenated with the aid of a Pd-containing catalyst in the presence of a small amount of water. A high yield and a high selectivity are obtained in a commercially attractive process. The reaction mixture obtained can without intermediate further processing be subjected to an oxidation in which the cinnamaldehyde is oxidized to 3-phenylpropionic acid with a high degree of conversion and a high selectivity. The combination of the two process steps constitutes a simple, commercially attractive process for the preparation of 3-phenylpropionic acid using cinnamaldehyde as a starting material. The resulting 3-phenyl-propionic acid product may serve as an intermediate reagent in the synthesis of anti-viral pharmaceuticals, particularly HIV protease inhibitors.
摘要翻译：制备3-苯基丙醛的方法，其中肉碱醛在少量水存在的情况下借助含Pd催化剂氢化。在商业上有吸引力的工艺中获得高产率和高选择性。所获得的反应混合物不经中间进一步处理，其中肉桂醛以高转化率和高选择性氧化成3-苯基丙酸。两个工艺步骤的组合构成了使用肉桂醛作为起始原料制备3-苯基丙酸的简单的，商业上有吸引力的方法。所得3-苯基 - 丙酸产物可用作合成抗病毒药物，特别是HIV蛋白酶抑制剂的中间试剂。

2. 发明授权

US5610268A Dendritic macromolecule and the preparation thereof 失效
标题翻译：树枝状大分子及其制备方法
公开(公告)号：US5610268A
公开(公告)日：1997-03-11
申请号：US486294
申请日：1995-06-07
申请人： Egbert W. Meijer , Hubertus J. M. Bosman , Franciscus H. A. M. J. Vandenbooren , Ellen M. M. De Brabander-Van Den Berg , Anna M. C. F. Castelijns , Hendrikus C. J. De Man , Rafael W. E. G. Reintjens , Christiaan J. C. Stoelwinder , Atze J. Nijenhuis
发明人： Egbert W. Meijer , Hubertus J. M. Bosman , Franciscus H. A. M. J. Vandenbooren , Ellen M. M. De Brabander-Van Den Berg , Anna M. C. F. Castelijns , Hendrikus C. J. De Man , Rafael W. E. G. Reintjens , Christiaan J. C. Stoelwinder , Atze J. Nijenhuis
IPC分类号： C08G73/02 , C08G83/00 , C08L101/00 , C09D201/00 , C08G63/44 , C08G73/00
CPC分类号： C08G83/003 , C08G73/0206 , C08G73/0213 , C08L101/005 , C09D201/005 , Y10S424/16
摘要： The invention relates to a dendritic macromolecule comprising a core and branches emanating from the core wherein the branches are based on vinyl cyanide and/or fumaryl dinatrile units. The invention also relates to processes for preparing these dendritic macromolecules. The dendritic macromolecules according to the invention are not sensitive to degradation through hydrolysis reactions and are also very stable at a high temperature. The processes are very suitable for large scale production of the dendritic macromolecules without requiring purification of reaction intermediates.
摘要翻译：本发明涉及一种树枝状大分子，其包含核心和从芯发出的分支，其中分支基于乙烯基氰化物和/或富马酰二腈单元。本发明还涉及制备这些树枝状大分子的方法。根据本发明的树枝状大分子对通过水解反应的降解不敏感，并且在高温下也非常稳定。该方法非常适合大规模生产树枝状大分子而不需要纯化反应中间体。

3. 发明授权

US5786507A Process for the preparation of 3-phenylpropionic acid 失效
标题翻译： 3-苯基丙酸的制备方法
公开(公告)号：US5786507A
公开(公告)日：1998-07-28
申请号：US834380
申请日：1997-04-16
申请人： Anna M. C. F. Castelijns , Johanna M. Hogeweg , Simon P. J. M. van Nispen
发明人： Anna M. C. F. Castelijns , Johanna M. Hogeweg , Simon P. J. M. van Nispen
IPC分类号： B01J23/44 , C07B61/00 , C07C45/62 , C07C51/235 , C07C57/30 , C07C51/16
CPC分类号： C07C45/62 , C07C51/235
摘要： Process for the preparation of 3-phenylpropionic acid in which 3-phenylpropanal is subjected to an oxidation, at elevated temperature, in particular at a temperature of between 40.degree. and 80.degree. C., using a medium containing molecular oxygen. A high degree of conversion and a high selectivity are obtained. The starting material 3-phenylpropanal can be prepared in a suitable manner through the hydrogenation of cinnamaldehyde in the presence of a Pd-containing catalyst, after which the reaction mixture obtained can without intermediate further processing be used in the oxidation reaction. The combination of the two process steps constitutes a simple, commercially attractive process for the preparation of 3-phenylpropionic acid using cinnamaldehyde as a starting material. 3-phenylpropionic acid can be used in particular in the preparation of pharmaceuticals such as HIV protease inhibitors.
摘要翻译：制备3-苯基丙酸的方法，其中3-苯基丙醛在升高的温度下，特别是在40℃至80℃的温度下，使用含有分子氧的培养基进行氧化。获得高转化率和高选择性。原料3-苯基丙醛可以通过在含Pd催化剂的存在下氢化肉桂醛以合适的方式制备，之后得到的反应混合物无需中间进一步处理即可用于氧化反应。两个工艺步骤的组合构成了使用肉桂醛作为起始原料制备3-苯基丙酸的简单的，商业上有吸引力的方法。 3-苯基丙酸特别可用于制备药物如HIV蛋白酶抑制剂。

4. 发明授权

US5616804A Process for the preparation of dibenzylamine 失效
标题翻译：二苄胺的制备方法
公开(公告)号：US5616804A
公开(公告)日：1997-04-01
申请号：US560510
申请日：1995-11-17
申请人： Anna M. C. F. Castelijns , Peter J. D. Maas
发明人： Anna M. C. F. Castelijns , Peter J. D. Maas
IPC分类号： C07C209/26 , C07C209/78
CPC分类号： C07C209/26
摘要： The present process involves preparing dibenzylamine through the hydrogenation of benzaldehyde in the presence of ammonia and a catalyst containing palladium using a small amount of solvent or dispersion medium. With the present process, dibenzylamine can be prepared with high selectivity in a relatively short reaction time and with complete conversion of the benzaldehyde, at which makes it commercially attractive. In the present process, a palladium-carbon catalyst is preferably used.
摘要翻译：本方法涉及通过使用少量溶剂或分散介质在氨的存在下通过苯甲醛的氢化和含钯的催化剂来制备二苄基胺。通过本发明方法，可以在相当短的反应时间内以及完全转化苯甲醛以高选择性制备二苄基胺，从而使其具有商业上的吸引力。在本方法中，优选使用钯 - 碳催化剂。

5. 发明授权

US5438143A Process for the preparation of substituted pyridines via 1-aza-1,3-butadienes and the 1-aza-1,3-butadiene intermediates 失效
标题翻译：通过1-氮杂-1,3-丁二烯和1-氮杂-1,3-丁二烯中间体制备取代吡啶的方法
公开(公告)号：US5438143A
公开(公告)日：1995-08-01
申请号：US983556
申请日：1993-05-21
申请人： Anna M. C. F. Castelijns , Henricus J. Arts
发明人： Anna M. C. F. Castelijns , Henricus J. Arts
IPC分类号： C07C251/12 , C07C251/14 , C07C251/16 , C07C251/40 , C07C317/26 , C07C323/23 , C07D213/08 , C07D213/09 , C07D213/12 , C07D215/06
CPC分类号： C07D213/08 , C07C251/16 , C07C251/40 , C07D213/09 , C07D213/12
摘要： Process for the preparation of substituted pyridines by allowing 1-aza-1,3-butadienes to react, in the presence of a catalytic amount of secondary amine and acid, with an aldehyde or ketone, and new 1-aza-1,3-butadienes which are used in this process. Said pyridines can be obtained in high yield in a simple process with a short reaction time. The 1-aza-1,3-butadiene can, if so desired, be prepared in situ from an imine and an aldehyde.
摘要翻译： PCT No.PCT / NL91 / 00148 Sec。 371日期：1993年5月21日 102（e）日期1993年5月21日PCT 1991年8月7日PCT PCT。公开号WO92 / 02505 日期1992年2月20日。通过使1-氮杂-1,3-丁二烯在催化量的仲胺和酸存在下与醛或酮反应制备取代吡啶的方法，以及新的1 在这个过程中使用的-aza-1,3-丁二烯。所述吡啶可以在短的反应时间的简单方法中以高产率获得。如果需要，1-氮杂-1,3-丁二烯可以由亚胺和醛原位制备。

6. 发明授权

US5254712A Process for the preparation of 5-oxohexane nitriles and the compound 2,4-dimethyl-5-oxohexane nitrile 失效
标题翻译： 5-氧代己烷腈和化合物2,4-二甲基-5-氧代己烷腈的制备方法
公开(公告)号：US5254712A
公开(公告)日：1993-10-19
申请号：US902785
申请日：1992-06-24
申请人： Anna M. C. F. Castelijns , Henricus J. Arts , Richard Green
发明人： Anna M. C. F. Castelijns , Henricus J. Arts , Richard Green
IPC分类号： C07C255/17 , C07D213/08 , C07C253/30
CPC分类号： C07D213/08 , C07C255/17
摘要： The invention relates to a process for the preparation of high yields of 5-oxohexane nitriles with minimum formation of 1 undesired isomer. Such nitriles may be utilized as starting materials for the preparation of pharmaceutical and agrochemical intermediates and as well as final products. The process comprises reacting a methyl ketone and an .alpha.,.beta.-unsaturated nitrile in the presence of a catalytically effective amount of a strong base. One of the products which may be created by the process is 2,4-dimethyl-5-oxohexane nitrile.
摘要翻译：本发明涉及一种制备高产量的5-氧代己烷腈的方法，最少形成1种不需要的异构体。这种腈可以用作制备药物和农药中间体以及最终产品的起始原料。该方法包括在催化有效量的强碱存在下使甲基酮和α，β-不饱和腈反应。可以通过该方法产生的产物之一是2,4-二甲基-5-氧代己烷腈。

7. 发明授权

US5824804A Method for the preparation of a N-alkoxy-(tetra-or hexahydro)-phthalimide and method for the preparation of a N-alkoxyamine 失效
标题翻译：制备N-烷氧基 - （四或六氢） - 邻苯二甲酰亚胺的方法及其制备方法
公开(公告)号：US5824804A
公开(公告)日：1998-10-20
申请号：US928126
申请日：1997-09-12
申请人： Joannes M. C. A. Mulders , Dominique M. C. Callant , Anna M. C. F. Castelijns
发明人： Joannes M. C. A. Mulders , Dominique M. C. Callant , Anna M. C. F. Castelijns
IPC分类号： C07D209/48
CPC分类号： C07D209/48 , Y02P20/582
摘要： Method for the preparation of N-alkoxy-(tetra- or hexahydro)-phthalimide according to formula I ##STR1## R.sub.1 being methyl or ethyl and R.sub.2 and R.sub.3 being each independently of one another hydrogen or alkyl with 1-4 C atoms or R.sub.2 and R.sub.3 together with the carbon atom to which they are bonded forming a ring with 5 or 6 C atoms, wherein the salt of the corresponding N-hydroxy-(tetrahydro- or hexahydro)-phthalimide according to formula II: ##STR2## with R.sub.2 and R.sub.3 as defined above and M being an alkali metal, is brought into contact with R.sub.1 Cl as alkylating agent, wherein R.sub.1 has the aforementioned meaning. The N-alkoxy-(tetra- or hexahydro)-phthalimide can afterwards be converted with the aid of hydroxylamine sulphate into the corresponding alkoxyamine after which the alkoxyamine obtained can be isolated. In this manner a simple and commercially attractive process for the preparation of O-(m)ethylhydroxylamine can be implemented.
摘要翻译：用于制备式I的N-烷氧基 - （四或六氢） - 邻苯二甲酰亚胺的方法，其中R 1和R 3各自独立地为氢或具有1-4个C原子的烷基或 R2和R3与它们所键合的碳原子一起形成具有5或6个C原子的环，其中根据式II的相应的N-羟基 - （四氢 - 或六氢） - 邻苯二甲酰亚胺的盐：其中R 1和R 3如上所定义，M是碱金属，与R1Cl作为烷基化剂接触，其中R1具有上述含义。 N-烷氧基 - （四或六氢） - 邻苯二甲酰亚胺可以随后借助于硫酸羟胺转化成相应的烷氧基胺，之后可以分离获得的烷氧基胺。以这种方式，可以实现用于制备O-（m）乙基羟胺的简单和商业上有吸引力的方法。

8. 发明授权

US5274165A Process for the .alpha.-chlorination of phenylacetonitriles 失效
标题翻译：苯乙腈的α-氯化方法
公开(公告)号：US5274165A
公开(公告)日：1993-12-28
申请号：US894430
申请日：1992-06-05
申请人： Anna M. C. F. Castelijns , Joannes M. C. A. Mulders , Cornelis W. van den Broek
发明人： Anna M. C. F. Castelijns , Joannes M. C. A. Mulders , Cornelis W. van den Broek
IPC分类号： C07C253/30 , C07C255/35
CPC分类号： C07C255/35
摘要： Process for the .alpha.-chlorination of phenylacetonitriles, for example benzyl cyanide, in which the phenylacetonitrile is contacted with a suitable chlorinating agent, sulphuryl chloride or chlorine gas, while an amount of strong acid, preferably HCl, is also present in the reaction mixture. The induction time and the reaction rate are dependent on, among other factors, the concentration of the acid. Preferably, the reaction is carried out under pressure. The reaction is well controllable.

9. 发明授权

US4649211A Process for the preparation of 2-cyanomethylcyclohexanone 失效
标题翻译： 2-氰基甲基环己酮的制备方法
公开(公告)号：US4649211A
公开(公告)日：1987-03-10
申请号：US649653
申请日：1984-09-12
申请人： Anna M. C. F. Castelijns , Thomas M. G. Aarts
发明人： Anna M. C. F. Castelijns , Thomas M. G. Aarts
IPC分类号： C07B61/00 , B01J27/00 , B01J27/26 , C07C67/00 , C07C253/00 , C07C255/46 , C07C120/00 , C07C121/46
CPC分类号： C07C255/00
摘要： The invention relates to a process for the preparation of 2-cyanomethylcyclohexanone by1. converting cyclohexanone to a Mannich base with a secondary amine salt and formaldehyde2. converting the Mannich base to the corresponding cyanohydrin with a cyanide3. pyrolysing the cyanohydrin obtained in step 2, wherein the pyrolysis of the cyanohydrin is carried out in the presence of a polar, aprotic solvent having a boiling point of more than 140.degree. C. and/or sodium cyanide.
摘要翻译：本发明涉及一种通过以下方法制备2-氰基甲基环己酮的方法：1.用仲胺盐和甲醛将环己酮转化为曼尼希碱。2.用氰化物将曼尼希碱转化为相应的氰醇3.热解步骤中获得的氰醇 2，其中氰醇的热解是在沸点高于140℃的极性非质子溶剂和/或氰化钠的存在下进行的。

10. 发明授权

US5663433A Process for the preparation N-alkyl-N,O-diacetyl hydroxylamine 失效
标题翻译：制备N-烷基-N，O-二乙酰羟胺的方法
公开(公告)号：US5663433A
公开(公告)日：1997-09-02
申请号：US668074
申请日：1996-06-17
申请人： Anna M. C. F. Castelijns , Joannes M. C. A. Mulders
发明人： Anna M. C. F. Castelijns , Joannes M. C. A. Mulders
IPC分类号： C07C259/06 , C07C231/00
CPC分类号： C07C259/06
摘要： Process for the preparation of N-alkyl-N,O-diacetyl hydroxylamine, for instance N-methyl-N,O-diacetyl hydroxylamine, by catalytic reduction of a nitroalkane, for instance nitromethane, in the presence of acetic anhydride. As catalyst preferably a platinum on alumina catalyst is used. The invention provides a simple one-step process for the preparation of N-alkyl-N,O-diacetyl hydroxylamine in a relatively concentrated reaction medium.
摘要翻译：在乙酸酐存在下，通过硝基烷烃例如硝基甲烷的催化还原来制备N-烷基-N，O-二乙酰基羟胺，例如N-甲基-N，O-二乙酰基羟胺的方法。作为催化剂，优选使用氧化铝上的催化剂。本发明提供了在相对浓缩的反应介质中制备N-烷基-N，O-二乙酰羟胺的简单的一步法。

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