公开(公告)号：US5412119A

公开(公告)日：1995-05-02

申请号：US11547

申请日：1993-02-01

申请人： Johannes Brussee ,  Arne van der Gen ,  Chris G. Kruse

发明人： Johannes Brussee ,  Arne van der Gen ,  Chris G. Kruse

IPC分类号： C07B53/00 ,  C07C213/00 ,  C07C215/04 ,  C07C215/24 ,  C07C215/34 ,  C07C217/08 ,  C07C217/70 ,  C07C233/36 ,  C07C253/30 ,  C07C255/26 ,  C07C311/05 ,  C07C317/28 ,  C07C323/25 ,  C07F7/18 ,  C07D315/00 ,  C07C215/00

CPC分类号： C07C217/70 ,  C07C213/00 ,  C07C215/24 ,  C07C215/34 ,  C07C217/08 ,  C07F7/184 ,  C07F7/1852 ,  C07F7/1892 ,  Y02P20/55

摘要： The present invention is concerned with the preparation of N-substituted vicinal aminoalcohol derivatives from the corresponding hydroxyl-protected cyanohydrin derivatives by successive partial reduction, transimination using a primary amine, reduction of the resulting imine and optional removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the starting cyanohydrin derivatives.The present invention is also concerned with certain new enantiomerically pure hydroxyl-protected vicinal aminoalcohols.

摘要翻译： 本发明涉及通过连续部分还原，使用伯胺进行转移，还原所得亚胺和任选除去羟基保护基，由相应的羟基保护的氰醇衍生物制备N-取代的连位氨基醇衍生物。 取决于起始羟腈衍生物的立体化学组成，产物以外消旋体或光学纯的形式获得。 本发明还涉及某些新的对映异构体纯的羟基保护的邻氨基醇。

公开(公告)号：US5189219A

公开(公告)日：1993-02-23

申请号：US810139

申请日：1991-12-19

申请人： Johannes Brussee ,  Arne van der Gen ,  Cornelis G. Kruse

发明人： Johannes Brussee ,  Arne van der Gen ,  Cornelis G. Kruse

IPC分类号： C07F7/18 ,  C07B53/00 ,  C07C213/00 ,  C07C213/02 ,  C07C215/30 ,  C07C215/52 ,  C07C215/60

CPC分类号： C07C213/02 ,  C07C213/00 ,  C07C215/30 ,  Y02P20/55

摘要： The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.

公开(公告)号：USRE35128E

公开(公告)日：1995-12-19

申请号：US255954

申请日：1994-06-07

申请人： Johannes Brussee ,  Arne van der Gen ,  Cornelis G. Kruse

发明人： Johannes Brussee ,  Arne van der Gen ,  Cornelis G. Kruse

IPC分类号： C07F7/18 ,  C07B53/00 ,  C07C213/00 ,  C07C213/02 ,  C07C215/30 ,  C07C215/52 ,  C07C215/60 ,  C07C209/52

CPC分类号： C07C213/02 ,  C07C213/00 ,  C07C215/30 ,  Y02P20/55

摘要： The present invention is concerned with the preparation of erythro N-substituted vicinal aminoalcohol derivatives from hydroxyl-protected cyanohydrin derivatives by successive Grignard reaction, transimination using a primary amine, reduction of the resulting imine and removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the cyanohydrin derivatives.

摘要翻译： 本发明涉及由羟基保护的氰醇衍生物通过连续格氏反应制备赤式N-取代的邻位氨基醇衍生物，使用伯胺进行转移，还原所得亚胺和除去羟基保护基。 取决于羟腈衍生物的立体化学组成，产物可以以外消旋体或光学纯的形式获得。