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1. 发明授权

US08106242B2 Process for the production of compounds via hazardous intermediates in a series of microreactors 有权
标题翻译：通过一系列微反应器中的危险中间体生产化合物的方法
公开(公告)号：US08106242B2
公开(公告)日：2012-01-31
申请号：US12301113
申请日：2007-05-23
申请人： Rafael Wilhelmus Elisabeth Ghislain Reintjens , Quirinus Bernardus Broxterman , Martina Kotthaus , Peter Poechlauer
发明人： Rafael Wilhelmus Elisabeth Ghislain Reintjens , Quirinus Bernardus Broxterman , Martina Kotthaus , Peter Poechlauer
IPC分类号： C07C209/42 , C07C45/40 , C07C29/132
CPC分类号： C07C29/132 , C07C45/40 , C07C45/517 , C07C45/53 , C07C209/42 , C07C247/04 , C07C47/546 , C07C211/27 , C07C33/20
摘要： Multi-step process for the preparation of compounds via hazardous intermediates comprising the steps of a) preparing in a microreactor a hazardous intermediate and b) optionally performing one or more reaction steps on the hazardous intermediate in one or more additional microreactors and c) further converting the hazardous intermediate with a suitable reaction agent in a subsequent microreactor until a stable end product is formed.
摘要翻译：用于通过有害中间体制备化合物的多步骤方法，包括以下步骤：a）在微反应器中制备危险中间体，和b）任选地在一种或多种另外的微反应器中对危险中间体进行一个或多个反应步骤，和c）进一步转化该危险中间体在随后的微反应器中具有合适的反应剂，直到形成稳定的最终产物。

2. 发明申请

US20110008852A1 CONVERGENT SYNTHESIS OF RENIN INHIBITORS AND INTERMEDIATES USEFUL THEREIN 失效
标题翻译：雷尼辛抑制剂和中间体的合成合成
公开(公告)号：US20110008852A1
公开(公告)日：2011-01-13
申请号：US12810220
申请日：2008-12-19
申请人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Boogers , Quirinus Bernardus Broxterman
发明人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Boogers , Quirinus Bernardus Broxterman
IPC分类号： C12P13/00 , C07C253/16 , C07C255/20 , C07F7/18 , C07D307/33 , C07C43/205
CPC分类号： C07D307/33 , C07C231/02 , C07C231/18 , C07D307/32 , C07F1/02 , C07F7/1804 , C07C237/22
摘要： Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3—6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).
摘要翻译：描述了制备肾素抑制剂如阿利吉仑的方法和其中有用的中间体。该方法引入含氮中间体如式（8）的内酯。其中R4是支链C 3-6烷基。在内酯或相关中间体的制备中，可以通过从满足式（10）的手性醛开始来控制所需的立体化学构型。

3. 发明申请

US20100304451A1 PROCESS FOR THE PREPARATION OF AN ENANTIOMERICALLY AND/OR DIASTEREOMERICALLY ENRICHED ESTER, THIOESTER, ALCOHOL OR THIOL 审中-公开
标题翻译：制备高效和/或二酯盐酸盐，硫醇，酒精或硫醇的方法
公开(公告)号：US20100304451A1
公开(公告)日：2010-12-02
申请号：US12682927
申请日：2008-10-15
申请人： Gerardus Karel Maria Verzijl , Peter Jan Leonard Mario Quaedflieg , Quirinus Bernardus Broxterman
发明人： Gerardus Karel Maria Verzijl , Peter Jan Leonard Mario Quaedflieg , Quirinus Bernardus Broxterman
IPC分类号： C12P17/12 , C12P11/00 , C12P7/62 , C12P17/10 , C12P17/04 , C07C319/02 , C07C27/02
CPC分类号： C12P7/6436 , C12P13/001 , C12P13/02 , C12P41/004
摘要： The invention relates to a process for preparing an enantiomerically and/or diastereomerically enriched ester or thioester having at least two adjacent chiral centres, wherein a mixture of stereoisomers of a secondary alcohol or thiol having a structure comprising a first chiral center forming a secondary alcohol or secondary thiol moiety in the beta position relative to a second chiral center having one hydrogen substituent, is reacted with an acyl donor in the presence of an epimerisation catalyst and a stereoselective acylation catalyst.
摘要翻译：本发明涉及一种制备具有至少两个相邻手性中心的对映异构体和/或非对映体富集的酯或硫酯的方法，其中仲醇或硫醇的立体异构体的混合物具有包含形成仲醇的第一手性中心或在相对于具有一个氢取代基的第二手性中心处于β位置的仲硫醇部分与酰基供体在差向异构化催化剂和立体选择性酰化催化剂存在下反应。

4. 发明授权

US06794542B2 Method for the preparation of enantiomerically enriched compounds 失效
标题翻译：制备对映体富集化合物的方法
公开(公告)号：US06794542B2
公开(公告)日：2004-09-21
申请号：US10148853
申请日：2002-10-09
申请人： Wilhelmus Hubertus Joseph Boesten , Harold Monro Moody , Bernardus Kaptein , Johannes Paulus Gerardus Seerden , Marcelles Van Der Sluis , Ben Lange De , Quirinus Bernardus Broxterman
发明人： Wilhelmus Hubertus Joseph Boesten , Harold Monro Moody , Bernardus Kaptein , Johannes Paulus Gerardus Seerden , Marcelles Van Der Sluis , Ben Lange De , Quirinus Bernardus Broxterman
IPC分类号： C07C23305
CPC分类号： C07C253/00 , C07B2200/07 , C07C209/62 , C07C227/32 , C07C231/06 , C07C231/18 , C07C253/08 , C07C253/30 , C07C229/08 , C07C233/06 , C07C237/20 , C07C255/25 , C07C255/43
摘要： Process for the preparation of a diasteromerically enriched phenylglycine amide derivative in which an enantiomerically enriched phenylglycine amide is converted into the corresponding Schiff base with the aid of compound R2—C(O)—R3, and the Schiff base obtained is subsequently converted into the diastereomerically enriched phenyglycine amide derivative with the aid of a cyanide source, a reducing agent or an allyl organometallic compound. The phenylglycine amide derivatives obtained are interesting starting materials for the preparation of for example enantiomerically enriched &agr;- and or &bgr;-amino acids and derivatives thereof, such as amides and esters, and amines.
摘要翻译：制备非对映体富集的苯基甘氨酸酰胺衍生物的方法，其中通过化合物R2-C（O）-R3将对映异构体富集的苯基甘氨酸酰胺转化成相应的希夫碱，随后将获得的席夫碱转化为非对映异构体在氰化物源，还原剂或烯丙基有机金属化合物的帮助下，富集的苯基甘氨酸酰胺衍生物。获得的苯基甘氨酸酰胺衍生物是用于制备例如对映体富集的α-和/或β-氨基酸及其衍生物如酰胺和酯以及胺的令人感兴趣的起始原料。

5. 发明授权

US08563279B2 Convergent synthesis of renin inhibitors and intermediates useful therein 失效
标题翻译：肾素抑制剂和其中有用的中间体的收敛合成
公开(公告)号：US08563279B2
公开(公告)日：2013-10-22
申请号：US12810220
申请日：2008-12-19
申请人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Franciscus Boogers , Quirinus Bernardus Broxterman
发明人： Ben De Lange , Anna Maria Cornelia Francisca Castelijns , Johannes Gerardus De Vries , Andreas Hendrikus Maria De Vries , Jeroen Antonius Franciscus Boogers , Quirinus Bernardus Broxterman
IPC分类号： C07C231/18 , C07C253/16 , C07C255/20 , C07F1/02 , C07F7/18 , C07D307/32 , C07D307/33 , C12P13/00
CPC分类号： C07D307/33 , C07C231/02 , C07C231/18 , C07D307/32 , C07F1/02 , C07F7/1804 , C07C237/22
摘要： Described is a method for the preparation of renin inhibitors such as aliskiren, and intermediates useful therein. The method introduces a nitrogen-containing intermediate such as a lactone of formula (8). with R4 being a branched C3—6 alkyl. In the preparation of the lactone, or related intermediates, a desired stereochemical configuration can be controlled by starting from a chiral aldehyde satisfying formula (10).
摘要翻译：描述了制备肾素抑制剂如阿利吉仑的方法和其中有用的中间体。该方法引入含氮中间体如式（8）的内酯。其中R4是支链C 3-6烷基。在内酯或相关中间体的制备中，可以通过从满足式（10）的手性醛开始来控制所需的立体化学构型。

6. 发明申请

US20080167500A1 Process for the Preparation of a Diastereomerically Enriched Compound 审中-公开
标题翻译：制备非对映异构体的化合物的方法
公开(公告)号：US20080167500A1
公开(公告)日：2008-07-10
申请号：US11632699
申请日：2005-07-20
申请人： Quirinus Bernardus Broxterman , Ben De Lange , Henrius Leonardus Marie Elsenberg , Matthias Weber
发明人： Quirinus Bernardus Broxterman , Ben De Lange , Henrius Leonardus Marie Elsenberg , Matthias Weber
IPC分类号： C07C211/01
CPC分类号： C07C209/28 , C07C2601/02 , C07C211/17 , C07C211/27 , C07C211/29
摘要： The present invention relates to a process for the preparation of a diastereomerically enriched compound, wherein a first compound according to formula (I), is contacted with a second compound according to formula (II), to form a third compound according to formula (III), whereby the compound according to formula (III) is subsequently reduced and thereby converted into a compound according to formula (IV), in which formulas: R1=a cycloalkyl group whereby R1 # R2, R2=a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenyl group, aryl group, cyclic or acyclic heteroalkyl group or heteroaryl group, R3=an alkyl group, R4=a substituted or unsubstituted: phenyl- or naphthyl-group, *=a chiral center. The invention furthermore relates to a diastereomerically enriched compound according to formula (IV) and its use in the preparation of pharmaceutical and agrochemically active compounds. The invention further relates to a process for the preparation of enantiomerically enriched compounds of formula (V), through hydrogenolysis of diastereomerically enriched compounds of formula (IV), wherein R1 and R2 have the meanings given above.
摘要翻译：本发明涉及一种制备非对映体富集的化合物的方法，其中根据式（I）的第一化合物与式（II）的第二化合物接触，以形成式（III）的第三化合物），由此将式（III）化合物随后还原，从而转化成式（Ⅳ）化合物，其中R 1 =环烷基，其中R 1 （环）烷基，（环）烯基，芳基，环状或无环杂烷基的取代或未取代的或杂芳基，R 3 =烷基，R 4 =取代或未取代的：苯基或萘基，* =手性中心。本发明还涉及根据式（IV）的非对映异构体富集的化合物及其在制备药物和农业化学活性化合物中的用途。本发明还涉及通过氢解非对映体富集的式（Ⅳ）化合物来制备对映体富集的式（Ⅴ）化合物的方法，其中R 1和R 2， SUB>具有上述含义。

7. 发明授权

US07371901B2 Process for the preparation of alkynols 失效
标题翻译：制备炔醇的方法
公开(公告)号：US07371901B2
公开(公告)日：2008-05-13
申请号：US10575757
申请日：2004-10-14
申请人： Quirinus Bernardus Broxterman , Gerardus Karel Maria Verzijl
发明人： Quirinus Bernardus Broxterman , Gerardus Karel Maria Verzijl
IPC分类号： C07C27/10 , C07C29/10 , C07C35/00
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—CH(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：其中R 2代表甲基，卤代甲基或乙基的具有式HC≡C-CH（OH）-R 2（式2）的炔醇的方法，其中相应的具有式1的甲硅烷基保护的炔醇酯，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 O >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，在水存在下和至少相当于胺官能团的量被转化为具有式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。

8. 发明授权

US07183443B2 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：US07183443B2
公开(公告)日：2007-02-27
申请号：US10510660
申请日：2003-04-07
申请人： Bernardus Henricus Nicolaas Dassen , Bernardus Kaptein , Quirinus Bernardus Broxterman
发明人： Bernardus Henricus Nicolaas Dassen , Bernardus Kaptein , Quirinus Bernardus Broxterman
IPC分类号： C07C45/44 , C07C29/48
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。

9. 发明申请

US20100029990A1 PROCESS FOR THE PRODUCTION OF COMPOUNDS VIA HAZARDOUS INTERMEDIATES IN A SERIES OF MICROREACTORS 有权
标题翻译：在一系列微生物中通过危险中间体生产化合物的方法
公开(公告)号：US20100029990A1
公开(公告)日：2010-02-04
申请号：US12301113
申请日：2007-05-23
申请人： Rafael Wilhelmus Elisabeth Ghislain Reintjens , Quirinus Bernardus Broxterman , Martina Kotthaus , Peter Poechlauer
发明人： Rafael Wilhelmus Elisabeth Ghislain Reintjens , Quirinus Bernardus Broxterman , Martina Kotthaus , Peter Poechlauer
IPC分类号： C07C209/42 , C07C45/00 , C07C29/132
CPC分类号： C07C29/132 , C07C45/40 , C07C45/517 , C07C45/53 , C07C209/42 , C07C247/04 , C07C47/546 , C07C211/27 , C07C33/20
摘要： Multi-step process for the preparation of compounds via hazardous intermediates comprising the steps of a) preparing in a microreactor a hazardous intermediate and b) optionally performing one or more reaction steps on the hazardous intermediate in one or more additional microreactors and c) further converting the hazardous intermediate with a suitable reaction agent in a subsequent microreactor until a stable end product is formed.
摘要翻译：用于通过有害中间体制备化合物的多步骤方法，包括以下步骤：a）在微反应器中制备危险中间体，和b）任选地在一种或多种另外的微反应器中对危险中间体进行一个或多个反应步骤，和c）进一步转化该危险中间体在随后的微反应器中具有合适的反应剂，直到形成稳定的最终产物。

10. 发明授权

US06841691B2 Process for the preparation of enantiomerically enriched esters and alcohols 失效
标题翻译：用于制备对映体富集的酯和醇的方法
公开(公告)号：US06841691B2
公开(公告)日：2005-01-11
申请号：US10296840
申请日：2001-05-21
申请人： Gerardus Karel Maria Verzijl , Johannes Gerardus Vries De , Quirinus Bernardus Broxterman
发明人： Gerardus Karel Maria Verzijl , Johannes Gerardus Vries De , Quirinus Bernardus Broxterman
IPC分类号： C07B53/00 , C07B55/00 , C07C29/143 , C07C33/20 , C12P41/00 , C11G3/00
CPC分类号： C12P41/004
摘要： Method for the preparation of an enantiomerically enriched ester, in which a mixture of the enantiomers of the corresponding secondary alcohol is subjected, in the presence of an acyl donor, to an enantioselective conversion in the presence of a racemisation catalyst upon which the ester is formed and an acyl donor residue is obtained, and in which the acyl donor residue is irreversibly removed from the phase in which the enantioselective conversion takes place. Preferably the enantioselective conversion is carried out enzymatically and a transfer hydrogenation catalyst is used as racemisation catalyst.The secondary alcohol can be formed in situ from the corresponding ketone, in the presence of a hydrogen donor. It is also possible to use a mixture of the secondary alcohol and the corresponding ketone as substrate.Preferably the acyl donor is chosen so that the acyl donor residue is converted in situ into another compound and/or the acyl donor residue is removed via distillation under reduced pressure.The enantiomerically enriched esters obtained can subsequently be converted into the corresponding enantiomerically enriched alcohols, which are desirable intermediate products in the preparation of liquid crystals, agro chemicals or pharmaceuticals.
摘要翻译：制备对映异构体富集的酯的方法，其中将相应的仲醇的对映异构体的混合物在酰基供体的存在下在形成酯的外消旋催化剂存在下进行对映选择性转化并且获得酰基供体残基，并且其中酰基供体残基从其中进行对映选择性转化的相不可逆地除去。优选地，对映选择性转化酶进行酶促转移氢化催化剂作为外消旋化催化剂。仲醇可以在氢供体存在下由相应的酮原位形成。还可以使用仲醇和相应的酮的混合物作为底物。优选地选择酰基供体，使得酰基供体残基原位转化成另一种化合物和/或通过蒸馏除去酰基供体残留物所得到的对映异构体富集的酯可以随后转化成相应的对映异构体富集的醇，这在制备液晶，农用化学品或药物中是理想的中间产物。

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