公开(公告)号：US20100256368A1

公开(公告)日：2010-10-07

申请号：US12742286

申请日：2008-11-12

Applicant: Benjamin List ,  Xu Cheng

Inventor： Benjamin List ,  Xu Cheng

IPC: C07D251/10

CPC classification number: C07D251/48

Abstract: A process for the synthesis of 3,6-dihydro-1,3,5-triazine derivatives is claimed wherein a biguanid is reacted with acetaldehyde in the presence of an inorganic and/or organic base. The process can be carried out at mild and therefore economical reaction conditions.

Abstract translation: 要求合成3,6-二氢-1,3,5-三嗪衍生物的方法，其中在无机和/或有机碱的存在下，双胍与乙醛反应。 该方法可以在温和且经济的反应条件下进行。

公开(公告)号：US08703940B2

公开(公告)日：2014-04-22

申请号：US12742286

申请日：2008-11-12

Applicant: Benjamin List ,  Xu Cheng

Inventor： Benjamin List ,  Xu Cheng

IPC: C07D251/18

CPC classification number: C07D251/48

Abstract: A process for the synthesis of 3,6-dihydro-1,3,5-triazine derivatives is claimed wherein a biguanid is reacted with acetaldehyde in the presence of an inorganic and/or organic base. The process can be carried out at mild and therefore economical reaction conditions.

Abstract translation: 要求合成3,6-二氢-1,3,5-三嗪衍生物的方法，其中在无机和/或有机碱的存在下，双胍与乙醛反应。 该方法可以在温和且经济的反应条件下进行。

公开(公告)号：US09079869B2

公开(公告)日：2015-07-14

申请号：US13203382

申请日：2010-03-02

Applicant: Benjamin List ,  Frank Lay ,  Pilar Garcia Garcia

Inventor： Benjamin List ,  Frank Lay ,  Pilar Garcia Garcia

IPC: A61K31/554 ,  C07D285/36 ,  C07D285/01

CPC classification number: C07D285/01

Abstract: Chiral disulfonimides having the formula I to III, wherein at least one of the groups A and B in the compound of formula I, C and D of the compound in formula II, and E and F of the compound in formula III is a chiral group, or E and F together form a chiral backbone, X is C, Si, O, N or S, and n is 0, 1, 2, 3, 4, 5 or 6, where n is >1 only if X is C, and G is as defined herein, and to the organic salts, metal salts and metal complexes thereof, are suited as NMR shift reagents and as reagents for racemate splitting, and also as chiral Brønsted acid catalysts or chiral Lewis acid catalysts for activating ketones, aldehydes and alkenes, and also as catalysts in the organic synthesis.

Abstract translation: 具有式I至III的手性二磺酰亚胺，其中式I化合物中的基团A和B中至少一个，式II化合物中的C和D，以及式III中化合物的E和F是手性基团 ，或E和F一起形成手性主链，X为C，Si，O，N或S，n为0,1,2,3,4,5或6，其中只有X为C时，n为> 1 和G如本文所定义，并且其有机盐，金属盐和金属络合物适合用作NMR位移试剂和用作外消旋体分裂的试剂，以及用作活化酮的手性布朗斯台德酸催化剂或手性路易斯酸催化剂， 醛和烯烃，以及有机合成中的催化剂。

公开(公告)号：US06268488B1

公开(公告)日：2001-07-31

申请号：US09318661

申请日：1999-05-25

Applicant: Carlos F. Barbas, III ,  Doron Shabat ,  Christoph Rader ,  Benjamin List ,  Richard A. Lerner

Inventor： Carlos F. Barbas, III ,  Doron Shabat ,  Christoph Rader ,  Benjamin List ,  Richard A. Lerner

IPC: C07H1524

CPC classification number: C07H15/252

Abstract: The present invention provides a compound that includes an active therapeutic agent attached to a blocking moiety that is sensitive to the catalytic action of molecules having retro-aldol and retro-Michael catalytic activity, methods for making such compounds and methods of converting such compounds to active therapeutic agents using molecules having aldolase activity.

Abstract translation: 本发明提供了一种化合物，其包含与对具有后 - 醛醇缩合反应的分子的催化作用敏感的阻断部分连接的活性治疗剂和复合迈克尔催化活性，制备这种化合物的方法和将这些化合物转化为活性的方法 使用具有醛缩酶活性的分子的治疗剂。

公开(公告)号：US08471046B2

公开(公告)日：2013-06-25

申请号：US12920877

申请日：2009-03-12

Applicant: Benjamin List ,  Corinna Reisinger ,  Xingwang Wang

Inventor： Benjamin List ,  Corinna Reisinger ,  Xingwang Wang

IPC: C07D301/12

CPC classification number: C07D301/12

Abstract: A process is claimed for the enantioselective epoxidation of α,β-unsaturated ketones, in which a compound of the general formula I, is reacted with an oxidizing agent to form α,β-epoxy ketones of the general formula II, in which R1, R2, R3 are as defined above. The α,β-epoxy ketones of the general formula II can be obtained in good yields and outstanding enantioselectivities from α,β-unsaturated ketones of the general formula I by epoxidation with hydrogen peroxide in the presence of a chiral catalyst, such as amino compounds and their acid addition salts.

Abstract translation: 要求对α，β-不饱和酮进行对映选择性环氧化的方法，其中通式I的化合物与氧化剂反应形成通式II的α，β-环氧酮，其中R1， R2，R3如上所定义。 通式II的α，β-环氧酮可以通过在手性催化剂如氨基化合物的存在下用过氧化氢进行环氧化，以良好的收率和通式I的α，β-不饱和酮的优异的对映选择性获得。 和它们的酸加成盐。

公开(公告)号：US20110313150A1

公开(公告)日：2011-12-22

申请号：US13203382

申请日：2010-03-02

Applicant: Benjamin List ,  Frank Lay ,  Pilar Garcia Garcia

Inventor： Benjamin List ,  Frank Lay ,  Pilar Garcia Garcia

IPC: C07D285/36

CPC classification number: C07D285/01

Abstract: Chiral disulfonimides having the formula I to III, wherein at least one of the groups A and B in the compound of formula I, C and D of the compound in formula II, and E and F of the compound in formula III is a chiral group, or E and F together form a chiral backbone, X is C, Si, O, N or S, and n is 0, 1, 2, 3, 4, 5 or 6, where n is >1 only if X is C, and G is as defined herein, and to the organic salts, metal salts and metal complexes thereof, are suited as NMR shift reagents and as reagents for racemate splitting, and also as chiral Brønsted acid catalysts or chiral Lewis acid catalysts for activating ketones, aldehydes and alkenes, and also as catalysts in the organic synthesis.

Abstract translation: 具有式I至III的手性二磺酰亚胺，其中式I化合物中的基团A和B中至少一个，式II化合物中的C和D，以及式III中化合物的E和F是手性基团 ，或E和F一起形成手性主链，X为C，Si，O，N或S，n为0,1,2,3,4,5或6，其中只有X为C时，n为> 1 和G如本文所定义，并且其有机盐，金属盐和金属络合物适合用作NMR位移试剂和用作外消旋体分裂的试剂，以及用作活化酮的手性布朗斯台德酸催化剂或手性路易斯酸催化剂， 醛和烯烃，以及有机合成中的催化剂。

公开(公告)号：US20090281346A1

公开(公告)日：2009-11-12

申请号：US12373955

申请日：2007-07-17

Applicant: Benjamin List ,  Michael Stadler ,  Jung Woon Yang

Inventor： Benjamin List ,  Michael Stadler ,  Jung Woon Yang

IPC: C07C271/18

CPC classification number: C07C269/06 ,  C07C271/18

Abstract: Disclosed is a method for producing aminocarbonyl compounds of the general formula (I) wherein R1 and R2 can be identical or different and represents hydrogen, alkyl, alkenyl, alkynyl, or aryl, X represents hydrogen, alkyl, alkenyl, alkynyl, aryl, or OR3, R3 representing hydrogen, alkyl, alkenyl, alkynyl, or aryl. According to said method, an aldehyde of the general formula (II) R1CO  (II) wherein R1 has the meaning indicated above, is reacted with an imine of the general formula (III) wherein R2 and X have the meaning indicated above, in the presence of a catalyst.Aminocarbonyles are obtained by means of catalyzed Mannich reactions with aldehydes. For example, if α-unbranched aldehydes are reacted with previously formed N-Boc imines in the presence of (S)-proline as a catalyst, the desired β-amino aldehydes are obtained at excellent yields, diastereoselectivities and enantioselectivities.

Abstract translation: 公开了一种制备通式（I）的氨基羰基化合物的方法，其中R 1和R 2可以相同或不同，表示氢，烷基，烯基，炔基或芳基，X表示氢，烷基，烯基，炔基，芳基或 OR3，R3代表氢，烷基，烯基，炔基或芳基。 根据所述方法，通式（II）的化合物R1CO（II）的醛，其中R1具有上述含义，与通式（Ⅲ）的亚胺反应，其中R2和X具有上述含义，在 存在催化剂。 氨基羰基通过与醛的催化曼尼希反应获得。 例如，如果在（S） - 脯氨酸作为催化剂的存在下使α-未分支的醛与先前形成的N-Boc亚胺反应，则获得所需的β-氨基醛，其产率优异，非对映选择性和对映选择性。

公开(公告)号：US20090182174A1

公开(公告)日：2009-07-16

申请号：US11575802

申请日：2005-09-27

Applicant: Benjamin List ,  Jung Woon Yang

Inventor： Benjamin List ,  Jung Woon Yang

IPC: C07C45/00

CPC classification number: C07C221/00 ,  C07C45/62 ,  C07C201/12 ,  C07C253/30 ,  C07C2601/14 ,  C07C47/277 ,  C07C47/21 ,  C07C49/86 ,  C07C47/02 ,  C07C47/228 ,  C07C223/06 ,  C07C255/56 ,  C07C205/44

Abstract: A method for the chemoselective hydrogenation of α, β unsaturated carbonyl compounds is disclosed, in which compounds of the formula R4R3C═CR2—C(O)R1, wherein R1-R4 are as defined herein, are reacted with a hybrid donor to form a compound of formula R4R3CH—CH(R2)—C(O)R1, in which R1-R4 are as above. That method permits the selective hydrogenation of α, β unsaturated aldehydes and ketones without the use of metal catalysts.

Abstract translation: 公开了用于α，β不饱和羰基化合物的化学选择性氢化的方法，其中式R 4 R 3 C-CR 2 -C（O）R 1（其中R 1 -R 4如本文所定义）的化合物与杂交供体反应形成 式R 4 R 3 CH-CH（R 2）-C（O）R 1的化合物，其中R 1 -R 4如上。 该方法允许α，β不饱和醛和酮的选择性氢化而不使用金属催化剂。

公开(公告)号：US06677435B2

公开(公告)日：2004-01-13

申请号：US09883758

申请日：2001-06-18

Applicant: Carlos F. Barbas, III ,  Doron Shabat ,  Christoph Rader ,  Benjamin List ,  Richard A. Lerner

Inventor： Carlos F. Barbas, III ,  Doron Shabat ,  Christoph Rader ,  Benjamin List ,  Richard A. Lerner

IPC: C07K1600

CPC classification number: C07H15/252

Abstract: The present invention provides a compound that includes an active therapeutic agent attached to a blocking moiety that is sensitive to the catalytic action of molecules having retro-aldol and retro-Michael catalytic activity, methods for making such compounds and methods of converting such compounds to active therapeutic agents using molecules having aldolase activity.

Abstract translation: 本发明提供了一种化合物，其包含与对具有后 - 醛醇缩合反应的分子的催化作用敏感的阻断部分连接的活性治疗剂和复合迈克尔催化活性，制备这种化合物的方法和将这些化合物转化为活性 使用具有醛缩酶活性的分子的治疗剂。

公开(公告)号：US20110009650A1

公开(公告)日：2011-01-13

申请号：US12920877

申请日：2009-03-12

Applicant: Benjamin List ,  Corinna Reisinger ,  Xingwang Wang

Inventor： Benjamin List ,  Corinna Reisinger ,  Xingwang Wang

IPC: C07D301/03

CPC classification number: C07D301/12

Abstract: A process is claimed for the enantioselective epoxidation of α,β-unsaturated ketones, in which a compound of the general formula I, is reacted with an oxidizing agent to form α,β-epoxy ketones of the general formula II, in which R1, R2, R3 are as defined above. The α,β-epoxy ketones of the general formula II can be obtained in good yields and outstanding enantioselectivities from α,β-unsaturated ketones of the general formula I by epoxidation with hydrogen peroxide in the presence of a chiral catalyst, such as amino compounds and their acid addition salts.

Abstract translation: 要求对α，bgr-不饱和酮的对映选择性环氧化方法，其中将通式I的化合物与氧化剂反应以形成通式II的α和b-环氧酮，其中 R1，R2，R3如上所定义。 通式II的α和bgr-环氧酮可以通过在手性催化剂存在下用过氧化氢进行环氧化，得到通式Ⅰ的α，bgr-不饱和酮的良好收率和优异的对映体选择性，例如 氨基化合物及其酸加成盐。