公开(公告)号：US20090298118A1

公开(公告)日：2009-12-03

申请号：US12083285

申请日：2006-10-19

申请人： Peter Jan Leonard Mario Quaedflieg ,  Theodorus Sonke ,  Gerardus Karel Maria Verzijl ,  Roel Wim Wiertz

发明人： Peter Jan Leonard Mario Quaedflieg ,  Theodorus Sonke ,  Gerardus Karel Maria Verzijl ,  Roel Wim Wiertz

IPC分类号： C12P21/00

CPC分类号： C12P21/00

摘要： The present invention relates to enzymatic oligopeptide synthesis in the N→C direction, in particular to a process for the preparation of an optionally N-protected oligopeptide C-terminal alkylester comprising the step of reacting the corresponding optionally N-protected oligopeptide C-terminal carboxyamide with an alkyl alcohol, preferably methanol, in the presence of a peptide amidase. The formed C-terminal alkylester can subsequently be used for the coupling with another amino acid residue or oligopeptide. Therefore, inventors have found a very advantageous process for the preparation of oligopeptides.

摘要翻译： 本发明涉及在N-> C方向的酶促寡肽合成，特别涉及制备任选N-保护的寡肽C端烷基酯的方法，该方法包括使相应的任选N-保护的寡肽C末端 羧酰胺与烷基醇，优选甲醇在肽酰胺酶存在下反应。 形成的C-末端烷基酯随后可用于与另一氨基酸残基或寡肽的偶联。 因此，发明人已经发现了制备寡肽的非常有利的方法。

公开(公告)号：US20080269529A1

公开(公告)日：2008-10-30

申请号：US11667381

申请日：2005-11-10

申请人： Johannes Gerardus (Hans) Vries De ,  Gerardus Karel Maria Verzijl ,  Andreas Hendrikus Maria Vries De ,  Vincent Ritleng ,  Adeline Marie Josephe Voelklin

发明人： Johannes Gerardus (Hans) Vries De ,  Gerardus Karel Maria Verzijl ,  Andreas Hendrikus Maria Vries De ,  Vincent Ritleng ,  Adeline Marie Josephe Voelklin

IPC分类号： C07F17/00 ,  C07C29/143

CPC分类号： C07F17/02

摘要： The invention relates to an enantiomerically enriched chiral compound comprising a transition metal M, which comprises four, five or six coordinating groups of which at least one pair is linked together to form a bidentate ligand, in which M is directly bound via one single σ-bond to a carbon atom of an optionally substituted and/or optionally fused (hetero)aromatic ring of said bidentate ligand and in which M is directly bound to a nitrogen atom of a primary or secondary amino group of said bidentate ligand, thereby forming a metallacycle between said bidentate ligand and the metal M, said metal M being selected from the metals of groups 8 and 9 of the Periodic Table of the Elements, in particular iron, ruthenium, osmium, cobalt, rhodium, or iridium. The chiral compound can be used as a catalyst, preferably in an asymmetric transfer hydrogenation process. The invention further relates to a process for an asymmetric transfer hydrogenation of a prochiral compound in the presence of a hydrogen donor and the chiral compound of the invention comprising a transition metal chosen from the metals of groups 8, 9 and 10 of the Periodic Table, in particular iron, ruthenium, osmium, cobalt, rhodium, iridium, nickel, palladium or platinum as the catalyst.

摘要翻译： 本发明涉及包含过渡金属M的对映异构体富集的手性化合物，其包含四个，五个或六个配位基团，其中至少一对连接在一起形成双齿配体，其中M通过一个单一的σ- 键合到所述二齿配位体的任选取代的和/或任选稠合的（杂）芳族环的碳原子，其中M直接与所述二齿配位体的伯或仲氨基的氮原子结合，由此形成金属环 在所述二齿配体和金属M之间，所述金属M选自元素周期表第8和9族的金属，特别是铁，钌，锇，钴，铑或铱。 手性化合物可以用作催化剂，优选在不对称转移氢化方法中。 本发明还涉及在氢供体和含有选自元素周期表第8,9和10族的金属的过渡金属的本发明的手性化合物的存在下前手性化合物的不对称转移氢化的方法， 特别是铁，钌，锇，钴，铑，铱，镍，钯或铂作为催化剂。

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。