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1. 发明授权

US4675418A Process for preparing alkanoic acids or esters thereof by rearrangement of alpha-halo-ketones in protic medium and in the presence of a non-noble metal salt 失效
标题翻译：通过在质子介质中和非贵金属盐存在下重排α-卤代酮来制备链烷酸或其酯的方法
公开(公告)号：US4675418A
公开(公告)日：1987-06-23
申请号：US398586
申请日：1982-07-15
申请人： Claudio Giordano , Giovanni Villa , Fulvio Uggeri , Graziano Castaldi
发明人： Claudio Giordano , Giovanni Villa , Fulvio Uggeri , Graziano Castaldi
IPC分类号： C07C67/475 , B01J27/00 , C07B31/00 , C07B41/00 , C07B41/08 , C07B41/12 , C07B61/00 , C07C45/63 , C07C49/84 , C07C51/00 , C07C57/30 , C07C59/64 , C07C67/00 , C07C69/612 , C07C69/734 , C07D333/24 , C07C63/36 , C07C69/76
CPC分类号： C07C45/63 , C07C49/84 , C07C51/00
摘要： Process for preparing alkanoic acid or their esters by rearrangement of alpha-halo-ketones in protic medium and in the presence of a non-noble metal salt.The protic medium is preferably an aliphatic alcohol having low molecular weight or water and the reaction is carried out at a temperature from 0.degree. C. to the boiling-point of the diluent or of the diluents mixture.
摘要翻译：通过在质子介质中和在非贵金属盐存在下重新配置α-卤代酮来制备链烷酸或其酯的方法。质子介质优选为具有低分子量或水的脂族醇，并且反应在0℃至稀释剂或稀释剂混合物的沸点的温度下进行。

2. 发明授权

US4734507A Optically active ketals, processes for their preparation and their use in the synthesis of alpha-arylalkanoic acids 失效
标题翻译：光学活性缩酮，其制备方法及其在α-芳基链烷酸合成中的应用
公开(公告)号：US4734507A
公开(公告)日：1988-03-29
申请号：US720379
申请日：1985-04-05
申请人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
发明人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
IPC分类号： A61K31/19 , A61K31/215 , A61K31/335 , A61K31/357 , A61P25/04 , A61P29/00 , C07B31/00 , C07B53/00 , C07B57/00 , C07C20060101 , C07C45/00 , C07C45/46 , C07C49/807 , C07C51/00 , C07C51/09 , C07C51/31 , C07C53/132 , C07C53/136 , C07C57/30 , C07C57/32 , C07C57/40 , C07C57/50 , C07C57/58 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/84 , C07C59/90 , C07C67/00 , C07C67/24 , C07C67/30 , C07C67/475 , C07C69/003 , C07C69/612 , C07C69/616 , C07C69/62 , C07C69/63 , C07C69/65 , C07C69/67 , C07C69/675 , C07C69/70 , C07C69/708 , C07C69/716 , C07C69/73 , C07C69/734 , C07C69/736 , C07C231/00 , C07C231/12 , C07C235/06 , C07C235/08 , C07C235/10 , C07C235/14 , C07C235/16 , C07C235/18 , C07C235/20 , C07C235/32 , C07D317/26 , C07D317/32 , C07D405/00 , C07D409/00 , C07D413/12 , C07D413/14 , C07D317/16 , C07D317/20 , C07D317/24
CPC分类号： C07D317/32 , C07C45/46 , C07C49/807 , C07C51/00
摘要： Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.4) alkyl group;X represents a chlorine, bromine or iodine atom, an hydroxy, acyloxy, alkylsulphonyloxy or arylsulphonyloxy group;the carbon atoms marked by an asterisk are both contemporaneously in the R or S configuration, are described.The preparation of the compound of formula I by ketalization or by trans-ketalization with tartaric acid derivatives and their rearrangement into alpha-arylalkanoic acids is described too.

3. 发明授权

US4697036A Process for the preparation of optically active alpha-arylalkanoic acids and novel intermediates thereof 失效
标题翻译：光学活性α-芳基链烷酸的制备方法及其新型中间体
公开(公告)号：US4697036A
公开(公告)日：1987-09-29
申请号：US720380
申请日：1985-04-05
申请人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
发明人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
IPC分类号： A61K31/19 , A61K31/215 , A61K31/335 , A61K31/357 , A61P25/04 , A61P29/00 , C07B31/00 , C07B53/00 , C07B57/00 , C07C20060101 , C07C45/00 , C07C45/46 , C07C49/807 , C07C51/00 , C07C51/09 , C07C51/31 , C07C53/132 , C07C53/136 , C07C57/30 , C07C57/32 , C07C57/40 , C07C57/50 , C07C57/58 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/84 , C07C59/90 , C07C67/00 , C07C67/24 , C07C67/30 , C07C67/475 , C07C69/003 , C07C69/612 , C07C69/616 , C07C69/62 , C07C69/63 , C07C69/65 , C07C69/67 , C07C69/675 , C07C69/70 , C07C69/708 , C07C69/716 , C07C69/73 , C07C69/734 , C07C69/736 , C07C231/00 , C07C231/12 , C07C235/06 , C07C235/08 , C07C235/10 , C07C235/14 , C07C235/16 , C07C235/18 , C07C235/20 , C07C235/32 , C07D317/26 , C07D317/32 , C07D405/00 , C07D409/00 , C07D413/12 , C07D413/14 , C07C51/16
CPC分类号： C07D317/32 , C07C45/46 , C07C49/807 , C07C51/00
摘要： A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represents a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group; the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a misture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids.
摘要翻译：描述了通过以下方法制备光学活性α-芳基链烷酸的新的对映选择性方法：（a）在缩酮的α-脂肪族碳原子上卤化式（ⅠA）的缩酮，其中Ar表示任选取代的芳基; R代表C1-C4烷基; R1和R2表示羟基，O-M +，OR3或NR4R5基团; 由星号表示的碳原子同时为（R）或（S）构型。这种反应是非对映选择性的，因此获得了一种α-卤代酮的混合物，其中两种差向异构体中的一种占优势，并且通常强烈地占优势。（b）通过式（IMA）的（C）（C）的酯，将单体或两个连续阶段中的X为Cl，Br或I的式（A）所示的配子重新排列成α-芳基链烷酸）化合物（A）和（C）都是新的化合物。重新布置步骤（b）可以在新的创造条件下进行。式（C）的酯具有类似于相应的α-芳基链烷酸的药理活性。

4. 发明授权

US4888433A Process for the preparation of optically active alpha-arylalkanoic acids and novel intermediates thereof 失效
标题翻译：光学活性α-芳基链烷酸的制备方法及其新型中间体
公开(公告)号：US4888433A
公开(公告)日：1989-12-19
申请号：US82196
申请日：1987-08-05
申请人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
发明人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
IPC分类号： A61K31/19 , A61K31/215 , A61K31/335 , A61K31/357 , A61P25/04 , A61P29/00 , C07B31/00 , C07B53/00 , C07B57/00 , C07C20060101 , C07C45/00 , C07C45/46 , C07C49/807 , C07C51/00 , C07C51/09 , C07C51/31 , C07C53/132 , C07C53/136 , C07C57/30 , C07C57/32 , C07C57/40 , C07C57/50 , C07C57/58 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/84 , C07C59/90 , C07C67/00 , C07C67/24 , C07C67/30 , C07C67/475 , C07C69/003 , C07C69/612 , C07C69/616 , C07C69/62 , C07C69/63 , C07C69/65 , C07C69/67 , C07C69/675 , C07C69/70 , C07C69/708 , C07C69/716 , C07C69/73 , C07C69/734 , C07C69/736 , C07C231/00 , C07C231/12 , C07C235/06 , C07C235/08 , C07C235/10 , C07C235/14 , C07C235/16 , C07C235/18 , C07C235/20 , C07C235/32 , C07D317/26 , C07D317/32 , C07D405/00 , C07D409/00 , C07D413/12 , C07D413/14
CPC分类号： C07D317/32 , C07C45/46 , C07C49/807 , C07C51/00
摘要： A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration. This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions. The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids.

5. 发明授权

US4579968A Process for the preparation of optically active alpha-arylalkanoic acids 失效
标题翻译：光学活性α-芳基链烷酸的制备方法
公开(公告)号：US4579968A
公开(公告)日：1986-04-01
申请号：US704406
申请日：1985-02-22
申请人： Graziano Castaldi , Claudio Giordano , Fulvio Uggeri
发明人： Graziano Castaldi , Claudio Giordano , Fulvio Uggeri
IPC分类号： C07C57/30 , C07B31/00 , C07B53/00 , C07B57/00 , C07C51/00 , C07C59/64 , C07C67/00 , C07C63/36
CPC分类号： C07C51/00
摘要： A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active (alpha-haloalkyl)-aryl-ketals and in submitting to hydrolysis the thus obtained esters of alpha-arylalkanoic acids. The rearrangement reaction is carried out under neutral or alightly alkaline conditions, in an aprotic dipolar diluent and in the presence of a protic substance having a high dielectric constant.
摘要翻译：公开了用于制备光学活性α-芳基链烷酸的方法，其组合在光学活性（α-卤代烷基） - 芳基缩酮的重排中，并且用于水解由此得到的α-芳基链烷酸的酯。重排反应在中性或弱碱性条件下进行，在非质子偶极稀释剂中和在具有高介电常数的质子物质存在下进行。

6. 发明授权

US4855464A Optically active ketals, processes for their preparation and their use in the synthesis of alpha-arylalkanoic acids 失效
标题翻译：光学活性缩酮，其制备方法及其在α-芳基链烷酸合成中的应用
公开(公告)号：US4855464A
公开(公告)日：1989-08-08
申请号：US134197
申请日：1987-12-17
申请人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
发明人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
IPC分类号： A61K31/19 , A61K31/215 , A61K31/335 , A61K31/357 , A61P25/04 , A61P29/00 , C07B31/00 , C07B53/00 , C07B57/00 , C07C20060101 , C07C45/00 , C07C45/46 , C07C49/807 , C07C51/00 , C07C51/09 , C07C51/31 , C07C53/132 , C07C53/136 , C07C57/30 , C07C57/32 , C07C57/40 , C07C57/50 , C07C57/58 , C07C59/52 , C07C59/56 , C07C59/64 , C07C59/84 , C07C59/90 , C07C67/00 , C07C67/24 , C07C67/30 , C07C67/475 , C07C69/003 , C07C69/612 , C07C69/616 , C07C69/62 , C07C69/63 , C07C69/65 , C07C69/67 , C07C69/675 , C07C69/70 , C07C69/708 , C07C69/716 , C07C69/73 , C07C69/734 , C07C69/736 , C07C231/00 , C07C231/12 , C07C235/06 , C07C235/08 , C07C235/10 , C07C235/14 , C07C235/16 , C07C235/18 , C07C235/20 , C07C235/32 , C07D317/26 , C07D317/32 , C07D405/00 , C07D409/00 , C07D413/12 , C07D413/14
CPC分类号： C07D317/32 , C07C45/46 , C07C49/807 , C07C51/00
摘要： Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## group, R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.4) alkyl group;X represents a chlorine, bromine or iodine atom, an hydroxy, acyloxy, alkylsulphonyloxy or arylsulphonyloxy group;the carbon atoms marked by an asterisk are both contemporaneously in the R or S configuration, are described.The preparation of the compound of formula I by ketalization or by trans-ketalization with tartaric acid derivatives and their rearrangement into alpha-arylalkanoic acids is decribed too.

7. 发明授权

US4582930A Process for the preparation of optically active alpha-arylalkanoic acids 失效
标题翻译：光学活性α-芳基链烷酸的制备方法
公开(公告)号：US4582930A
公开(公告)日：1986-04-15
申请号：US704407
申请日：1985-02-22
申请人： Graziano Castaldi , Claudio Giordano , Fulvio Uggeri
发明人： Graziano Castaldi , Claudio Giordano , Fulvio Uggeri
IPC分类号： C07C57/30 , C07B31/00 , C07B53/00 , C07C27/02 , C07C51/00 , C07C51/09 , C07C59/64 , C07C67/00 , C07C63/36
CPC分类号： C07C51/00
摘要： A process is disclosed for the preparation of optically active alpha-arylalkanoic acids, consisting in the rearrangement of optically active alpha-(haloalkyl)-aryl-ketals and in submitting to hydrolysis the so-obtained esters of alpha-arylalkanoic acids.The rearrangement reaction is carried out under neutral or slightly alkaline conditions in a polar protic medium.
摘要翻译：公开了用于制备光学活性α-芳基链烷酸的方法，其包括光学活性α-（卤代烷基） - 芳基缩酮的重排，并且将所得的α-芳基链烷酸酯进行水解。重排反应在极性质子介质中在中性或弱碱性条件下进行。

8. 发明授权

US4810819A Process for the preparation of optically active alpha-acrylalkanoic acids and novel intermediates thereof 失效
标题翻译：制备光学活性α-丙烯酰基链烷酸的方法及其新型中间体
公开(公告)号：US4810819A
公开(公告)日：1989-03-07
申请号：US81688
申请日：1987-08-05
申请人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
发明人： Claudio Giordano , Graziano Castaldi , Fulvio Uggeri , Silvia Cavicchioli
IPC分类号： C07C45/46 , C07C49/807 , C07C51/00 , C07D317/32 , C07C69/76
CPC分类号： C07D317/32 , C07C45/46 , C07C49/807 , C07C51/00
摘要： A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represents a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration. This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.The esters of formula (C) have pharmacological activity analogous to that of the corresponding alpha-arylalkanoic acids.
摘要翻译：描述了通过以下方法制备光学活性α-芳基链烷酸的新的对映选择性方法：（a）在缩酮的α-脂肪族碳原子上卤化式（ⅠA）的缩酮，其中Ar表示任选取代的芳基; R代表C1-C4烷基; R1和R2表示羟基，O-M +，OR3或NR4R5基团; 由星号表示的碳原子同时为（R）或（S）构型。该反应是非对映选择性的，因此获得了α-二酮的混合物，其中两个差向异构体中的一个占优势，并且通常强大地占优势。（b）通过式（IMA）的（C）（C）的酯，将单体或两个连续阶段中的X为Cl，Br或I的式（A）所示的配子重新排列成α-芳基链烷酸）化合物（A）和（C）都是新的化合物。重新布置步骤（b）可以在新的创造条件下进行。式（C）的酯具有类似于相应的α-芳基链烷酸的药理活性。

9. 发明授权

US4620031A Process for preparing alpha-aryl-alkanoic acids 失效
标题翻译：制备α-芳基 - 链烷酸的方法
公开(公告)号：US4620031A
公开(公告)日：1986-10-28
申请号：US697449
申请日：1985-02-01
申请人： Fulvio Uggeri , Graziano Castaldi , Claudio Giordano
发明人： Fulvio Uggeri , Graziano Castaldi , Claudio Giordano
IPC分类号： C07B41/08 , C07C51/00 , C07C57/30 , C07C57/32 , C07C57/58 , C07C59/64 , C07C59/84 , C07C67/00 , C07D333/24 , C07C63/36
CPC分类号： C07D333/24 , C07C51/00
摘要： Alpha-alkyl-alkanoic acids are prepared by heating at boiling temperature a mixture of an alpha-halogen-alkyl-arylketone in a saturated aliphatic diol or in a mixture of saturated aliphatic diols in the presence of a Broensted's acid and by successively alkalifying the reaction mixture.
摘要翻译： α-烷基 - 链烷酸通过在沸石温度下加热饱和脂肪族二醇中的α-卤代烷基 - 芳基酮或饱和脂族二醇的混合物，在布朗斯台德酸的存在下并通过连续碱化反应来制备混合物。

10. 发明授权

US4748253A Process for preparing esters of alkanoic acids via rearrangement of alpha-haloketals 失效
标题翻译：通过α-卤代酮重排制备链烷酸酯的方法
公开(公告)号：US4748253A
公开(公告)日：1988-05-31
申请号：US329333
申请日：1981-12-10
申请人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
发明人： Claudio Giordano , Aldo Belli , Fulvio Uggeri , Giovanni Villa
IPC分类号： C07C43/174 , C07C43/225 , C07C43/30 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07C67/475 , C07C69/734 , C07D209/48 , C07D317/16 , C07D317/18 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/16 , C07D333/22 , C07D333/24 , C07C69/76
CPC分类号： C07D209/48 , C07C43/303 , C07C43/315 , C07C45/63 , C07C51/00 , C07C59/64 , C07D317/16 , C07D317/22 , C07D317/28 , C07D319/06 , C07D333/22
摘要： Process for preparing esters of alkanoic acids via rearrangement of alpha-haloketals in the presence of a Lewis acid.The rection is preferably carried out in the presence of catalytic amounts of a Lewis acid and of a diluent at a temperature in the range from about 0.degree. to the reflux temperature of diluent.The esters thus obtained are useful as intermediate products for preparing drugs.The process involves the preparation of new alpha-haloketals.

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