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1.发明授权Method of preparing optically active alcohols which consist substantially or entirely of one enantiomer 失效制备基本上或完全由一种对映异构体组成的光学活性醇的方法
公开(公告)号：US5329023A
公开(公告)日：1994-07-12
申请号：US899026
申请日：1992-06-15
申请人： Johannes Brussee , Arne Van Der Gen
发明人： Johannes Brussee , Arne Van Der Gen
IPC分类号： C07C45/00 , C07C45/67 , C07C49/245 , C07C49/255 , C07C215/30 , C07F7/18 , C07C209/48
CPC分类号： C07C255/00 , C07C45/004 , C07C45/673 , C07C49/245 , C07C49/255 , C07F7/1852 , Y02P20/55
摘要： The invention relates to a method of preparing optically active alcohols which consist substantially (at least 75% e.e.) or entirely of one enantiomer of formula 4 ##STR1## wherein R and A are as defined therein. The method comprises, which maintaining enantiomeric excess, converting an optically active cyanohydrin of formula 1 ##STR2## into optically active protected cyanohydrin of formula 2 ##STR3## converting the protected cyanohydrin of formula 2 into an optically active compound of formula 3 ##STR4## removing the protecting group B.
摘要翻译： 本发明涉及一种制备光学活性醇的方法，其基本上（至少75％e.e。）或完全由式4（4）的对映异构体组成，其中R和A如其中所定义。 该方法包括保持对映异构体过量，将式1的光学活性羟考酮（1）转化成式2的光学活性保护的氰醇（2）将式2的被保护的氰醇转化为 （3）除去保护基团B.
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公开(公告)号：US5189219A
公开(公告)日：1993-02-23
申请号：US810139
申请日：1991-12-19
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.
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公开(公告)号：US5493047A
公开(公告)日：1996-02-20
申请号：US161420
申请日：1993-12-06
IPC分类号： C07C253/30 , C07C253/32 , C07C255/14 , C07C255/16 , C07C255/36 , C07C255/38
CPC分类号： C07C253/30 , C07B2200/07
摘要： The invention relates to a method of preparing an optically active cyanohydrin carboxylic acid ester from an optically active cyanohydrin of opposite configuration, wherein said starting cyanohydrin is converted with a carboxylic acid in the presence of a dialkyl azodicarboxylate and a triarylphosphine.The invention also relates to a method of preparing an optically active cyanohydrin of opposite configuration by a subsequent solvolysis of the ester obtained under conservation of the configuration.
摘要翻译： 本发明涉及由相对构型的光学活性羟腈制备光学活性羟腈羧酸酯的方法，其中所述起始氰醇在偶氮二羧酸二烷基酯和三芳基膦存在下用羧酸转化。 本发明还涉及一种制备相对构型的光学活性羟考醇的方法，该方法是通过在保持该构型后获得的酯的随后溶剂解作用。
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公开(公告)号：USRE35128E
公开(公告)日：1995-12-19
申请号：US255954
申请日：1994-06-07
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。
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公开(公告)号：US5412119A
公开(公告)日：1995-05-02
申请号：US11547
申请日：1993-02-01
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。
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