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1. 发明申请

US20050215822A1 Process for the preparation of enantiomerically enriched compounds 失效
标题翻译：制备富含对映体的化合物的方法
公开(公告)号：US20050215822A1
公开(公告)日：2005-09-29
申请号：US10510660
申请日：2003-04-07
申请人： Bernardus Hedricus Dassen , Bernardus Kaptein , Quirinus Broxterman
发明人： Bernardus Hedricus Dassen , Bernardus Kaptein , Quirinus Broxterman
IPC分类号： C07C29/48 , C07C213/08 , C07C221/00
CPC分类号： C12P13/02 , C07B2200/07 , C07C213/00 , C07C221/00 , C12P13/001 , C07C215/08 , C07C223/02
摘要： Process for the preparation of enantiomerically enriched amino aldehydes and amino alcohols, wherein a corresponding enantiomerically enriched amino nitrile is subjected to hydrogenation in the presence of hydrogen, a hydrogenation catalyst, preferably a Pd-catalyst and a mineral acid. For the preparation of an amino aldehyde hydrogen preferably is present at a hydrogen-pressure between 0.1 and 2 MPa, in particular between 0.5 and 1 MPa. The amino aldehyde preferably is isolated in the form of a chemically and configurationally stable derivative. For the preparation of an amino alcohol, preferably at least during part of the hydrogenation hydrogen is present at a hydrogen-pressure between 2 and 10 MPa, in particular between 4 and 6 MPa. In a preferred embodiment the hydrogen-pressure initially is between 0.5 and 2 MPa and subsequently, after most of the nitrile starting material is converted, the hydrogen pressure is increased to a value between 2 and 10 MPa. The enantiomerically enriched nitrile starting material may a.o. be prepared by enzymatic resolution, classical resolution, resolution via preferential crystallization, diastereomeric synthesis, catalytic asymmetric synthesis or dehydratation of amino acid amides.
摘要翻译：用于制备对映异构体富集的氨基醛和氨基醇的方法，其中相应的对映异构体富集的氨基腈在氢气，氢化催化剂，优选Pd-催化剂和无机酸的存在下进行氢化。对于氨基醛的制备，氢优选以0.1至2MPa，特别是0.5至1MPa的氢压存在。氨基醛优选以化学和结构稳定的衍生物的形式分离。对于氨基醇的制备，优选至少在部分氢化过程中，氢气的压力为2至10MPa，特别是4至6MPa。在一个优选的实施方案中，氢气压力最初为0.5-2MPa，随后在大部分腈起始原料转化后，氢气压力增加至2MPa至10MPa。对映异构体富集的腈起始物质可以是通过酶解，经典拆分，优化结晶，非对映体合成，催化不对称合成或氨基酸酰胺脱水制备。

2. 发明申请

US20050107468A1 Process for the preparation of an enantiomerically enriched thio compound 审中-公开
标题翻译：用于制备对映体富集的硫代化合物的方法
公开(公告)号：US20050107468A1
公开(公告)日：2005-05-19
申请号：US10498924
申请日：2002-12-02
申请人： Thijs Kuilman , Quirinus Broxterman , Gerardus Verzijl , Henricus Martinus Straatman
发明人： Thijs Kuilman , Quirinus Broxterman , Gerardus Verzijl , Henricus Martinus Straatman
IPC分类号： C07C327/32 , A61K31/21 , A61K31/401 , A61K31/455 , C07B53/00 , C07B61/00 , C07C323/22 , C07D213/46
CPC分类号： C07C327/32
摘要： The invention relates to a process for the preparation of an enantiomerically enriched compound of formula (1) or a salt thereof, in which R1 and R2 each independently represent an (hetero)alkyl or (hetero)aryl group, wherein R1—C(O)—SH or a salt thereof, with R1 as defined above, is reacted with R2—C(C═CH2)—C(O)OH with R2 as defined above, wherein the reaction takes place in the presence of catalyst is an enantiomerically enriched Lewis acid containing a transition metal chosen from the group of Ti, Zr and Hf or a combination thereof and at least one enantiomerically enriched ligand, and in the presence of an alkali metal ion, an alkaline earth metal ion or an ammonium ion.
摘要翻译：本发明涉及一种制备对映体富集的式（1）化合物或其盐的方法，其中R 1和R 2各自独立地表示（杂原子）烷基或（杂）芳基，其中R 1 -C（O）-SH或其与如上定义的R 1'的盐与R 如上所定义的具有R 2的C（O）OH（C-CH 2）-C（O）OH，其中反应发生在存在催化剂是含有选自Ti，Zr和Hf的过渡金属或其组合的至少一种对映异构体富集的配体的对映异构体富集的路易斯酸，并且在碱金属离子存在下，碱土金属离子或铵离子。

3. 发明申请

US20070276150A1 Process for the Preparation of Alkynols 失效
标题翻译：制备炔醇的方法
公开(公告)号：US20070276150A1
公开(公告)日：2007-11-29
申请号：US10575757
申请日：2004-10-14
申请人： Quirinus Broxterman , Gerardus Karel Verzijl
发明人： Quirinus Broxterman , Gerardus Karel Verzijl
IPC分类号： C07F7/02
CPC分类号： C12P7/04 , C07C29/00 , C07C29/095 , C12P9/00 , C12P41/007 , C07C33/042
摘要： Process for the preparation of an alkynol with formula HC═C—C(OH)—R2 (formula 2) wherein R2 represents methyl, halomethyl or ethyl, wherein the corresponding silyl-protected alkynol ester with formula 1 wherein R1 represents H, or an optionally substituted alkyl, an optionally substituted alkenyl or an optionally substituted (hetero)aryl group, R2 is as defined above and A3Si represents a trisubstituted silyl group wherein each A independently represents an optionally substituted alkyl or an optionally substituted (hetero)aryl group, in the presence of water and at least an equivalent amount of amine functionalities is converted into the alkynol with formula 2. Preferably, the amount of water is between 0.5 and 3 equivalents calculated with respect to the amount of silyl-protected alkynol ester with formula (1).
摘要翻译：制备具有式HC-CC（OH）-R 2（式2）的炔醇的方法，其中R 2表示甲基，卤代甲基或乙基，其中相应的甲硅烷基其中R 1表示H，或任选取代的烷基，任选取代的烯基或任选取代的（杂）芳基，R 2是保护的炔醇，其中R 1表示H，或如上所定义，并且A 3 Si表示三取代的甲硅烷基，其中每个A独立地表示任选取代的烷基或任选取代的（杂）芳基，在水的存在下和至少等量的胺官能团被转化为具有式2的炔醇。优选地，相对于式（1）的甲硅烷基保护的炔醇酯的量，水的量为0.5-3当量。

4. 发明申请

US20060142610A1 Process for the racemisation of enantiomerically enriched alpha-amino nitriles 审中-公开
标题翻译：对映体富集的α-氨基腈外消旋化的方法
公开(公告)号：US20060142610A1
公开(公告)日：2006-06-29
申请号：US10535510
申请日：2003-11-03
申请人： Gerardus Verzijl , Bernardus Kaptein , Quirinus Broxterman
发明人： Gerardus Verzijl , Bernardus Kaptein , Quirinus Broxterman
IPC分类号： C07C253/30 , C12P13/00
CPC分类号： C07C253/30 , C07C255/24 , C07C255/42 , C07C255/44
摘要： Process for the racemisation of an enantiomerically enriched α-amino nitrile characterized in that the enantiomerically enriched α-amino nitrile is contacted with a lewis acid catalyst. Preferably an aprotic solvent is used. The lewis acid catalyst preferably comprises a metal chosen from main group elements IA-IVA of the Periodic Table (CAS version), the transition metals and the lanthanides, in particular Al, Ti, Zr, or lanthanides. The catalsyt for example has the general structure MnXpSqLr, and preferably is chosen from the group of aluminum alkoxides, aluminum alkyls, lanthanide alkoxydes and lanthanocenes. The racemisation may be performed in combination with a resolution process, for instance in combination with an enzymatic or a crystallization induced resolution process, preferably in situ, for instance in situ in a crystallization induced asymmetric transformation process.
摘要翻译：对映异构体富集的α-氨基腈的外消旋化方法，其特征在于对映异构体富集的α-氨基腈与路易斯酸催化剂接触。优选使用非质子溶剂。路易斯酸催化剂优选包含选自元素周期表主要元素IA-IVA（CAS版）的金属，过渡金属和镧系元素，特别是Al，Ti，Zr或镧系元素。例如，催化剂具有MnXpSqLr的一般结构，优选选自烷氧基铝，烷基铝，镧系烷氧基化物和镧系元素。外消旋化可以与分辨方法结合进行，例如与酶或结晶诱导的分辨方法组合进行，优选原位，例如在结晶诱导的非对称转化过程中原位。

5. 发明申请

US20070142657A1 Process for the preparation of aliphatic primary alcohols and intermediates in such process 审中-公开
标题翻译：在此过程中制备脂族伯醇和中间体的方法
公开(公告)号：US20070142657A1
公开(公告)日：2007-06-21
申请号：US10578687
申请日：2004-11-17
申请人： Georgios Sarakinos , Quirinus Broxterman
发明人： Georgios Sarakinos , Quirinus Broxterman
IPC分类号： C07F7/00
CPC分类号： C07C29/10 , C07C31/02 , C07C43/166 , C07F7/1804 , Y02P20/55
摘要： The invention relates to protected unsaturated alcohol with formula (R1—O)mPG, wherein R1 represents a linear, straight-chain aliphatic hydrocarbon group containing one or more double bonds and having 26-30 C-atoms, m is 1 or 2 and PG, forming an ether group in combination with the —O— of the former primary alcohol, represents a protecting group chosen from the group of substituted methyl ethers, substituted ethyl ethers, (substituted) benzyl ethers and (substituted) silyl ethers with at least one substituent on the Si-atom being not a methyl group, in case m=1; and a diol protecting group in case m=2; A protected saturated alcohol with formula (R2—O—)mPG, herein R2 represents a linear straight-chain alkyl group with 26-30 C-atoms and PG and m are as defined above; unsaturated alcohols with formula R1OH wherein R1 represents a linear, straight-chain aliphatic hydrocarbon group containing one, two or three double bonds and having 27 C-atoms, a linear, straight-chain aliphatic hydrocarbon group containing one or more double bonds and having 28 C-atoms with the proviso that when R1 has one double bond which is between C18 and C19 or between C19 and C20, R1OH has the E-configuration, or a linear, straight-chain aliphatic hydrocarbon group containing two or three double bonds and having 26-29 C-atoms. The invention further relates to processes for the preparation of such protected unsaturated alcohols via an organometallic cross coupling reaction, a Wittig reaction via Olefin Cross Metathesis.
摘要翻译：本发明涉及具有式（R 1 -O-O）m PG的保护的不饱和醇，其中R 1表示直链的直链脂族含有一个或多个双键并具有26-30个碳原子的烃基，m为1或2，与前一个伯醇的-O-一起形成醚基的PG代表选自以下基团的保护基：在取代的甲基醚，取代的乙基醚，（取代的）苄基醚和（取代的）甲硅烷基醚与Si原子上的至少一个取代基不是甲基的情况下，m = 1; 在m = 2的情况下为二醇保护基; 具有式（R 2 -O -O））M的保护的饱和醇，其中R 2表示直链的直链烷基，其中26 -30个C原子和PG和m如上所定义; 具有式R 1 OH的不饱和醇其中R 1表示含有一个，两个或三个双键并具有27个C原子的直链的直链脂族烃基，一个含有一个或多个双键且具有28个C原子的直链，直链脂族烃基，条件是当R 1具有一个双键时，和C 19或C 19和C 20之间，R 1 OH具有E构型，或含有两个或三个双键且具有26-29个C原子的直链，直链脂族烃基。本发明还涉及通过有机金属交叉偶联反应制备这种受保护的不饱和醇的方法，通过烯烃交叉复分解的维蒂希反应。

6. 发明申请

US20070123589A1 Method for producing chiral or enantiomer-enriched beta-amino acids, aldehydes, ketones and gama-amino alcohols 审中-公开
标题翻译：制备手性或对映体富集的β-氨基酸，醛，酮和氨基醇的方法
公开(公告)号：US20070123589A1
公开(公告)日：2007-05-31
申请号：US10582671
申请日：2004-11-25
申请人： Walther Jary , Ben De Lange , Quirinus Broxterman , Peter Pochlauer , Marcellas Van Der Sluis , Patrick Uiterweerd , Heinz Falk , Gerhard Zuckerstatter
发明人： Walther Jary , Ben De Lange , Quirinus Broxterman , Peter Pochlauer , Marcellas Van Der Sluis , Patrick Uiterweerd , Heinz Falk , Gerhard Zuckerstatter
IPC分类号： A61K31/195 , A61K31/13 , C07C227/02
CPC分类号： C07C213/00 , C07C231/12 , Y02P20/55 , C07C215/28 , C07C233/18 , C07C233/31 , C07C233/47
摘要： The invention relates to an improved method for producing chiral or enantiomer-enriched beta amino acids, -aldehydes, -ketones and gamma-amino alcohols, during which an allyl amine of formula (I), in which: R1 represents an alkyl radical, a cycloalkyl radical, an alkyl radical, a heterocycle radical or a condensed or bridged ring system; R2, R3, R4 and R5, independent of one another, can represent H or an alkyl radical, a cyclo alkyl radical, an aryl radical, a heterocycle radical or a condensed or bridged ring system or radicals R1, R2, R3 and R4, together, form ring systems that can optionally contain one or more heteroatoms, whereby radicals R1, R2, R3, R4 and R5 can be substituted once or a number of times, and; R6 represents H or an N-protective group, is transformed; a) by ozonolysis in a solvent and; b) subsequent decomposition of the peroxide-containing solution by means of an oxidizing agent or reductive reprocessing, into the corresponding amino compound of formula (II), in which R1, R2, R3, R4 and R6 are defined as above, and; A, according to the reprocessing, represents a radical of formula COOH, —C(OH)R5 or —C(O)R5, whereby R5 is defined as above.
摘要翻译：本发明涉及制备手性或对映体富集的β氨基酸，醛，酮和γ-氨基醇的改进方法，其中式（I）的烯丙胺，其中：R1表示烷基，环烷基，烷基，杂环基或稠合或桥连环系; R 2，R 3，R 4和R 5彼此独立地可以表示H或烷基，环烷基，芳基，杂环基或稠合或桥接的环系或基团R 1，R 2，R 3和R 4，一起形成可任选地含有一个或多个杂原子的环系，其中基团R 1，R 2，R 3，R 4和R 5可以被取代一次或多次， R6表示H或N-保护基，被转化; a）通过溶剂中的臭氧分解; b）随后通过氧化剂或还原再加工将含过氧化物的溶液分解成相应的式（II）的氨基化合物，其中R 1，R 2，R 3，R 4和R 6如上定义; 根据后处理，A代表式COOH，-C（OH）R 5或-C（O）R 5的基团，其中R 5如上所定义。

7. 发明申请

US20070083058A1 Process for the preparation of aliphatic primary alcohols and related intermediates in such process 审中-公开
标题翻译：在此过程中制备脂族伯醇和相关中间体的方法
公开(公告)号：US20070083058A1
公开(公告)日：2007-04-12
申请号：US10578671
申请日：2004-11-17
申请人： Georgios Sarakinos , Quirinus Broxterman
发明人： Georgios Sarakinos , Quirinus Broxterman
IPC分类号： C07F7/00 , C07C43/02
CPC分类号： C07C43/174 , C07C43/164 , C07D309/12 , C07F7/1804 , Y02P20/55
摘要： The invention relates to protected alcohol with formula (R1—O—)mPG, wherein R1 represents a linear, straight-chain alkyl group having 26-30 C-atoms, m is 1 or 2, and PG, forming an ether group in combination with the —O— of the former primary alcohol, represents a protecting group chosen from the group of substituted methyl, substituted ethyl, substituted benzyl and (substituted) silyl groups with at least one substituent on the Si-atom being not a methyl group, in case m=1; and a diol protecting group in case m=2, with the proviso that PG is no saccharide. The invention further relates to process for the preparation of such protected alcohols via an organometallic cross coupling reaction.
摘要翻译：本发明涉及具有式（R 1 -O -OM）m PG的保护的醇，其中R 1表示直链的直链烷基具有26-30个碳原子的基团，m为1或2，与前一个伯醇的-O-结合形成醚基的PG代表选自取代的甲基，取代的乙基，在m = 1的情况下，在Si原子上具有至少一个取代基的取代的苄基和（取代的）甲硅烷基不是甲基; 在m = 2的情况下为二醇保护基，条件是PG不是糖。本发明还涉及通过有机金属交叉偶联反应制备这种被保护的醇的方法。

8. 发明申请

US20060135790A1 Process for the preparation of an alpha-amino carbonyl compound 审中-公开
标题翻译：制备α-氨基羰基化合物的方法
公开(公告)号：US20060135790A1
公开(公告)日：2006-06-22
申请号：US10546212
申请日：2004-03-04
申请人： David Hyett , Daniel Mink , Quirinus Broxterman , Bernardus Kaptein , Hubertus Zeegers
发明人： David Hyett , Daniel Mink , Quirinus Broxterman , Bernardus Kaptein , Hubertus Zeegers
IPC分类号： C07D207/02
CPC分类号： C07C231/02 , C07C249/02 , C07C253/30 , C07C237/16 , C07C251/08 , C07C251/24 , C07C255/28 , C07C255/61
摘要： The invention relates to a process for the preparation of an α-amino carbonyl compound by reacting an imine starting material with a suitable electrophile in the presence of a base. This process has the advantage that the imine starting materials can be prepared from glyoxylic acid esters or glyoxylic acid ester derivatives and α-hydrogen containing primary amines, which are usually cheap and readily available. These imine starting materials can usually be prepared with a high yield and/or almost without the formation of any side products.
摘要翻译：本发明涉及通过在碱存在下使亚胺起始原料与合适的亲电子试剂反应来制备α-氨基羰基化合物的方法。该方法的优点在于，亚胺原料可以由乙醛酸酯或乙醛酸酯衍生物和含α-伯氢的伯胺制备，通常便宜且易于获得。这些亚胺原料通常可以以高产率和/或几乎不形成任何副产物来制备。

9. 发明申请

US20060122430A1 Process for the preparation of an enantiomerically enriched schiff base 审中-公开
标题翻译：用于制备对映异构体富集的席夫碱的方法
公开(公告)号：US20060122430A1
公开(公告)日：2006-06-08
申请号：US10534737
申请日：2003-11-03
申请人： Alexander Duchateau , Ronald Gebhard , Quirinus Broxterman
发明人： Alexander Duchateau , Ronald Gebhard , Quirinus Broxterman
IPC分类号： C07C209/78
CPC分类号： C07D317/30 , C07C249/02
摘要： Process for the preparation of an enantiomerically enriched Schiff base wherein an amine is contacted with a carbonyl compound wherein the amine and/or the carbonyl compound is a chiral compound, to form a mixture of the enantiomers of the corresponding Schiff base wherein, if the amine is the chiral compound the carbonyl compound is an aromatic aldehyde; if the carbonyl compound is the chiral compound the amine is an aromatic amine and if both the amine and the carbonyl compound are chiral compounds, they in combination may have the same meanings as given above for both the chiral amine and the chiral carbonyl compound situation, and the mixture of enantiomers of the Schiff base is subjected to preparative chromatography on a stationary phase whereby separation of the enantiomers of the Schiff base is obtained. Preferably chiral Simulated Moving Bed chromatography is used.
摘要翻译：制备对映异构体富集席夫碱的方法，其中胺与羰基化合物接触，其中胺和/或羰基化合物是手性化合物，以形成相应希夫碱的对映异构体的混合物，其中如果胺是手性化合物，羰基化合物是芳族醛; 如果羰基化合物是手性化合物，则胺是芳族胺，如果胺和羰基化合物都是手性化合物，它们的组合可以具有与手性胺和手性羰基化合物情况相同的含义，并将席夫碱的对映异构体的混合物在固定相上进行制备色谱，由此获得希夫碱的对映异构体的分离。优选使用手性模拟移动床层析法。

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