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1. 发明授权

US4973696A Stereoselective process for preparing optically active alpha, beta-disubstituted carbonyl compounds 失效
标题翻译：用于制备光学活性α，β-二取代羰基化合物的立体选择性方法
公开(公告)号：US4973696A
公开(公告)日：1990-11-27
申请号：US297387
申请日：1989-01-17
申请人： Claudio Giordano , Graziano Castaldi , Silvia Cavicchioli , Francesco Minisci
发明人： Claudio Giordano , Graziano Castaldi , Silvia Cavicchioli , Francesco Minisci
IPC分类号： C07B53/00 , C07B31/00 , C07C45/00 , C07C45/57 , C07C45/59 , C07C45/63 , C07C45/78 , C07C47/02 , C07C47/52 , C07C67/00 , C07D317/30 , C07D317/32 , C07D493/08
CPC分类号： C07D493/08 , C07C45/59 , C07C45/63 , C07D317/32
摘要： A stereoselective process is described for preparing optically active alpha,beta-disubstituted carbonyl compounds, comprising forming an acetal between an alpha,beta-unsaturated aldehyde or ketone and tartaric acid or a derivative thereof, halogenating the product thus obtained, and restoring the carbonyl compound.
摘要翻译：描述了制备光学活性α，β-二取代羰基化合物的立体选择性方法，包括在α，β-不饱和醛或酮与酒石酸或其衍生物之间形成缩醛，卤化所得产物，还原羰基化合物。

2. 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.

3. 发明授权

US4764642A Process for preparing optically active alpha-haloalkyl-aryl-ketones 失效
标题翻译：制备光学活性α-卤代烷基 - 芳基酮的方法
公开(公告)号：US4764642A
公开(公告)日：1988-08-16
申请号：US915573
申请日：1986-10-06
申请人： Graziano Castaldi , Silvia Cavicchioli , Claudio Giordano
发明人： Graziano Castaldi , Silvia Cavicchioli , Claudio Giordano
IPC分类号： C07B31/00 , C07B53/00 , C07C45/00 , C07C45/59 , C07C49/80 , C07C49/84 , C07C67/00 , C07D317/32
CPC分类号： C07C49/80 , C07C45/59 , C07C49/84 , C07D317/32
摘要： A process is described for preparing alpha-haloalkyl-aryl-ketones, comprising reacting a substantially anhydrous strong acid with a ketal of formula ##STR1## in which Ar, R, R.sub.1, R.sub.2 and X have the meanings given in the description.
摘要翻译：描述了制备α-卤代烷基 - 芳基酮的方法，包括使基本上无水的强酸与式（I）的缩酮反应，其中Ar，R，R 1，R 2和X具有在说明书中给出的含义。

4. 发明授权

US5284966A Intermediates for the stereochemical inversion of (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R) enantiomers 失效
标题翻译：（2S，3S）-2-氨基-3-苯基-1,3-丙二醇在其（2R，3R）对映异构体中立体化学反转的中间体
公开(公告)号：US5284966A
公开(公告)日：1994-02-08
申请号：US992747
申请日：1992-12-18
申请人： Marco Villa , Claudio Giordano , Silvia Cavicchioli , Silvio Levi
发明人： Marco Villa , Claudio Giordano , Silvia Cavicchioli , Silvio Levi
IPC分类号： C07C315/04 , C07B55/00 , C07C55/00 , C07C213/08 , C07C213/10 , C07C215/30 , C07C215/34 , C07C215/36 , C07C315/06 , C07C317/32 , C07C319/20 , C07C319/26 , C07C323/32 , C07C323/39 , C07C323/41 , C07C323/42 , C07C323/43 , C07D263/06 , C07C381/00 , C07C321/00 , C07C323/00
CPC分类号： C07C323/39 , C07C317/32 , C07C323/32 , C07D263/06
摘要： Intermediates for transforming (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R)-enantiomers are described. The final compounds are useful intermediates for the synthesis of antibiotics like Chloramphenicol, Thiamphenicol and Florfenicol.
摘要翻译：描述了将（2S，3S）-2-氨基-3-苯基-1,3-丙二醇转化成其（2R，3R） - 对映异构体的中间体。最终的化合物是合成抗生素如氯霉素，甲砜霉素和氟苯尼考的有用中间体。

5. 发明授权

US5202484A Process for the stereochemical inversion of (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R) enantiomers 失效
标题翻译：（2S，3S）-2-氨基-3-苯基-1,3-丙二醇在其（2R，3R）增效剂中的立体化学反应的方法
公开(公告)号：US5202484A
公开(公告)日：1993-04-13
申请号：US599881
申请日：1990-10-19
申请人： Marco Villa , Claudio Giordano , Silvia Cavicchioli , Silvio Levi
发明人： Marco Villa , Claudio Giordano , Silvia Cavicchioli , Silvio Levi
IPC分类号： C07C315/04 , C07B55/00 , C07C55/00 , C07C213/08 , C07C213/10 , C07C215/30 , C07C215/34 , C07C215/36 , C07C315/06 , C07C317/32 , C07C319/20 , C07C319/26 , C07C323/32 , C07C323/39 , C07C323/41 , C07C323/42 , C07C323/43 , C07D263/06
CPC分类号： C07C323/39 , C07C317/32 , C07C323/32 , C07D263/06
摘要： A four step process for transforming (2S,3S)-2-amino-3-phenyl-1,3-propanediols into their (2R,3R)-enantiomers is described. The final compounds are useful intermediates for the synthesis of antibiotics like Chloramphenicol, Thiamphenicol and Florfenicol. The starting products generally are discard products in the synthesis of said antibiotics.

6. 发明授权

US5084569A Trioxy bicyclic compounds useful for preparing optically active carboxylic acids 失效
标题翻译：用于制备光学活性羧酸的三元双环化合物
公开(公告)号：US5084569A
公开(公告)日：1992-01-28
申请号：US493752
申请日：1990-03-15
申请人： Marco Villa , Claudio Giordano , Graziano Castaldi , Silvia Cavicchioli
发明人： Marco Villa , Claudio Giordano , Graziano Castaldi , Silvia Cavicchioli
IPC分类号： B01J31/02 , C07B31/00 , C07B41/08 , C07B53/00 , C07B61/00 , C07C51/00 , C07C57/30 , C07C59/64 , C07C67/00 , C07D317/32 , C07D493/08
CPC分类号： C07D493/08 , C07C51/00 , C07D317/32
摘要： A stereoconvergent process is described for preparing optically active alpha-arylalkanoic acids using as starting substance a diastereoisomeric mixture of ketals of formula ##STR1## in which the substitutents have the meanings given in the description. The described process leads to the formation of a single enantiomer.

7. 发明授权

US4937334A Process for the preparation of intermediates for the synthesis of diltiazem 失效
标题翻译：制备用于合成地尔硫卓的中间体的方法
公开(公告)号：US4937334A
公开(公告)日：1990-06-26
申请号：US384730
申请日：1989-07-25
申请人： Silvia Cavicchioli , Maurizio Paiocchi , Claudio Giordano
发明人： Silvia Cavicchioli , Maurizio Paiocchi , Claudio Giordano
IPC分类号： A61K31/554 , C07D281/10
CPC分类号： C07D281/10
摘要： A process for the preparation of the compound (2S,3S)(+)-3-hydroxy-2,3-dihydro-2-(4-methoxyphenyl)-5-(2-dimethylaminoethyl)-1, 5-benzothiazepin-4(5H)-one is described. Said compound is an intermediate useful in the synthesis of Diltiazem.

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

US4922009A Stereoconvergent process for preparing optically active carboxylic acids 失效
标题翻译：用于制备光学活性羧酸的立体选择性方法
公开(公告)号：US4922009A
公开(公告)日：1990-05-01
申请号：US137000
申请日：1987-12-23
申请人： Marco Villa , Claudio Giordano , Graziano Castaldi , Silvia Cavicchioli
发明人： Marco Villa , Claudio Giordano , Graziano Castaldi , Silvia Cavicchioli
IPC分类号： B01J31/02 , C07B31/00 , C07B41/08 , C07B53/00 , C07B61/00 , C07C51/00 , C07C57/30 , C07C59/64 , C07C67/00 , C07D317/32 , C07D493/08
CPC分类号： C07D493/08 , C07C51/00 , C07D317/32
摘要： A stereoconvergent process is described for preparing optically active alpha-arylalkanoic acids using as starting substance a diastereoisomeric mixture of ketals of formula ##STR1## in which the substituents have the meanings given in the description. The described process leads to the formation of a single enantiomer.

10. 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.

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