公开(公告)号：US06232314B1

公开(公告)日：2001-05-15

申请号：US09180258

申请日：1999-03-18

申请人： Bevyn Jarrott ,  Philip Mark Beart ,  William Roy Jackson ,  Vijaya Bhaskar Kenche ,  Alan Duncan Robertson ,  Maree Patricia Collis

发明人： Bevyn Jarrott ,  Philip Mark Beart ,  William Roy Jackson ,  Vijaya Bhaskar Kenche ,  Alan Duncan Robertson ,  Maree Patricia Collis

IPC分类号： C07D295092

CPC分类号： C07D295/185 ,  C07D213/38 ,  C07D295/092 ,  C07D307/81 ,  C07D311/58 ,  C07D317/58 ,  C07D333/28

摘要： Arylalkylpiperazine compounds (1) wherein B is aryl or optionally substituted aryl; R1 is hydroxy; R2 and R3 are the same or different and are independently selected from hydrogen or C1-3 alkyl; m is 0, 1 or 2; D is a linking chain of atoms which may be optionally substituted and which contains from 1 to 8 atoms in the chain; E is a phenolic antioxidant group or a corresponding amino derivative thereof wherein the phenolic hydroxyl is replaced by amino, are disclosed. The compounds have both free radical scavenging activity and block excitatory amino acid activity. Some compounds of the present invention also display an affinity for voltage-sensitive sodium channels.

公开(公告)号：US06187918B1

公开(公告)日：2001-02-13

申请号：US09523046

申请日：2000-03-10

申请人： William A. Nugent

发明人： William A. Nugent

IPC分类号： C07D295092

CPC分类号： C07D295/084

摘要： Novel chiral aminoalcohol catalysts and methods for their preparation are provided. The first catalyst is prepared via selective hydrogenation of one of two benzene rings in a precursor. The aminoalcohol promotes the asymmetric addition of organozinc reagents to aldehydes to afford optically active alcohols or their esters. The second catalyst is prepared by selective dialkylation of 3-exo-aminoisoborneol with a 2-haloethyl ether. The aminoalcohol promotes the addition of organozinc reagents to aliphatic aldehydes containing a &bgr;-branch with greatly enhanced enantioselectivity relative to DAIB.

摘要翻译： 提供了新的手性氨基醇催化剂及其制备方法。 通过前体中两个苯环之一的选择性氢化制备第一催化剂。 氨基醇促进有机锌试剂对醛的不对称加成，得到光学活性醇或其酯。 第二种催化剂是通过3-异 - 氨基异硼烷与2-卤代乙基醚的二烷基化来制备的。 氨基醇促进有机锌试剂添加到含有β-分支的脂族醛中，相对于DAIB具有极大增强的对映体选择性。