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1. 发明公开

EP0274277A2 A process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives 失效
标题翻译： Verfahren zur enzymematischen Trennung der optischen Isomere von racmischen Oxazolidinon-Derivaten。
公开(公告)号：EP0274277A2
公开(公告)日：1988-07-13
申请号：EP87311519.0
申请日：1987-12-30
申请人： Montedison S.p.A.
发明人： Cesti, Pietro , Bianchi, Daniele , Francalanci, Franco , Cabri, Walter
IPC分类号： C12P17/14 , C12P41/00
CPC分类号： C12P17/14 , C12P41/004
摘要： A process for the separation of a racemic mixture of the S(+) and R(-) optical isomers of an oxazolidinone compound of the formula:
(in which R is a straight or branched C₁-C₈ alkyl group) which process comprises reacting the racemic 3-alkyl-5-hydroxy-methyl-oxazolidin-2-one derivative of formula (I) with an esterifying compound which is

(a) an ester of the formula:
(in which Rʹ is a straight or branched C₁-C₁₀ alkyl or alkenyl group, and Rʺ is a straight or branched C₁-C₄ alkyl or alkenyl group, a haloalkyl group or a diacylglycerolic group),
(b) an acid of the formula:

Rʺʹ-COOH (V)

(in which Rʺʹ is a straight or branched C₁-C₂₀ alkyl or alkenyl group) or
(c) an anhydride of the formula:
(in which R IV is a straight or branched C₁-C₆ alkyl group)
the reaction being carried out in the presence of an enzyme, immobilized on a porous carrier, capable of selectively giving rise to the esterification of the R(-) isomer, while leaving the S(+) isomer of the racemic starting compound of formula (I) substantially unchanged;
and separating the S(+) isomer.
摘要翻译：分离下式的恶唑烷酮化合物的S（+）和R（ - ）旋光异构体的外消旋混合物的方法：其中R是直链或支链的C 1 -C 8烷基（其中R是直链或支链的C 1 -C 8烷基）包括使式（I）的外消旋的3-烷基-5-羟基 - 甲基 - 恶唑烷-2-酮衍生物与（a）下式的酯的酯化化合物反应（其中R'为直链或支链C 1 -C 10烷基或烯基，R“为直链或支链C 1 -C 4烷基或烯基，卤代烷基或二酰基甘油基），（b）下式的酸：R” -COOH（V）（其中R“'是直链或支链C 1 -C 20烷基或烯基）或（c）下式的酸酐：其中R IV是直链或支链 C1-C6烷基），该反应在固定在多孔载体上的酶存在下进行，其能够选择性地引起R（ - ）异构体的酯化，同时留下R（ - ）异构体的S（+）异构体外消旋的式（I）的起始化合物基本上不变; 并分离S（+）异构体。 >

2. 发明授权

EP0274277B1 A process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives 失效
标题翻译：一种用于区分氧化亚砷酸衍生物的光学异构体的酶分离的方法
公开(公告)号：EP0274277B1
公开(公告)日：1993-01-27
申请号：EP87311519.0
申请日：1987-12-30
申请人： Montedison S.p.A.
发明人： Cesti, Pietro , Bianchi, Daniele , Francalanci, Franco , Cabri, Walter
IPC分类号： C12P17/14 , C12P41/00
CPC分类号： C12P17/14 , C12P41/004

3. 发明公开

EP0274277A3 A process for the enzymatic separation of the optical isomers of racemic oxazolidinonic derivatives 失效
标题翻译：一种用于环氧亚烷基二胺衍生物的光学异构体的酶分离的方法
公开(公告)号：EP0274277A3
公开(公告)日：1989-06-14
申请号：EP87311519.0
申请日：1987-12-30
申请人： Montedison S.p.A.
发明人： Cesti, Pietro , Bianchi, Daniele , Francalanci, Franco , Cabri, Walter
IPC分类号： C12P17/14 , C12P41/00
CPC分类号： C12P17/14 , C12P41/004
摘要： A process for the separation of a racemic mixture of the S(+) and R(-) optical isomers of an oxazolidinone compound of the formula:
(in which R is a straight or branched C₁-C₈ alkyl group) which process comprises reacting the racemic 3-alkyl-5-hydroxy-methyl-oxazolidin-2-one derivative of formula (I) with an esterifying compound which is
(a) an ester of the formula:
(in which Rʹ is a straight or branched C₁-C₁₀ alkyl or alkenyl group, and Rʺ is a straight or branched C₁-C₄ alkyl or alkenyl group, a haloalkyl group or a diacylglycerolic group), (b) an acid of the formula:
Rʺʹ-COOH (V)
(in which Rʺʹ is a straight or branched C₁-C₂₀ alkyl or alkenyl group) or (c) an anhydride of the formula:
(in which R IV is a straight or branched C₁-C₆ alkyl group)
the reaction being carried out in the presence of an enzyme, immobilized on a porous carrier, capable of selectively giving rise to the esterification of the R(-) isomer, while leaving the S(+) isomer of the racemic starting compound of formula (I) substantially unchanged;
and separating the S(+) isomer.

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