摘要:
A 1-substituted-2-diphenylphosphinonaphthalene represented by formula (I): ##STR1## wherein at least one of R.sup.1, R.sup.2, R.sup.3, and R.sup.4, which may be the same or different, represents a lower alkyl group having 1 to 4 carbon atoms which may be substituted with an alkoxy group, a phenyl group or --OR.sup.6 (wherein R.sup.6 represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms or an alcohol-protective group), and the rest of them represent a hydrogen atom; A represents a single bond or a methylene group; and R.sup.5 represents a substituted or unsubstituted phenyl group; and a transition metal complex comprising the 1-substituted-2-diphenylphosphinonaphthalene as a ligand. The transition metal complex is useful as a catalyst in asymmetric synthesis.
摘要:
A process for preparing an optically active carnitine ester represented by formula (I): wherein R represents a lower alkyl group; and X represents a halogen atom, is disclosed, comprises asymmetrically hydrogenating a &ggr;-trimethylammonium-3-oxobutanoic ester halide represented by formula (II): wherein R and X are as defined above, in the presence of a ruthenium-optically active phosphine complex as a catalyst. An optically active carnitine ester of any desired isomerism can be obtained through simple operation in high yield at high optical purity. The substrate used is easily available.
摘要:
Disclosed herein is a process for producing a (2S,5S)-2,5-diamino-1,6-diphenyl-3-hexanone derivative represented by the formula (1): ##STR1## wherein R.sup.1 means a lower alkylcarbonyl group, a halogen-substituted lower alkylcarbonyl group, an arylcarbonyl group or a lower alkoxycarbonyl group, and R.sup.2 and R.sup.3 are identical with or different from each other and denote individually an aryl group or an alkoxy-substituted aryl group, which comprises subjecting a (2S)-2,5-diamino-1,6-diphenyl-4-hexen-3-one derivative represented by the formula (2): ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the same meaning as defined above, to a hydrogenation reaction in the presence of a transition metal-containing catalyst.
摘要:
A process for preparing a 4-acyloxyazetidinone or a derivative thereof represented by formula (IV): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a hydroxyethyl group, or a protected hydroxyethyl group; R.sup.3 represents an alkyl group having from 1 to 10 carbon atoms which may be substituted with a halogen atom, a cyano group, a lower alkoxy group or a phenyl group, or a substituted or unsubstituted phenyl group, provided that the .alpha.-positioned carbon atom of said alkyl group should not have more than two halogen atoms; and R.sup.4 represents a hydrogen atom, a lower alkyl group, or a lower alkoxycarbonyl group, which is useful as an intermediate for penem antibiotics is disclosed, comprising reacting azetidinone or a derivative thereof represented by formula (II): ##STR2## wherein R.sup.1 is as defined above, and R.sup.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group, or a carboxyl group, with a carboxylic acid represented by formula (III):R.sup.3 COOH (III)wherein R.sup.3 is as defined above, in the presence of (1) a transition metal compound selected from a ruthenium compound, an osmium compound, and a cobalt compound, (2) an aldehyde having 2 or more carbon atoms, provided that the carbon atom at the .alpha.-position thereof should not have two or more halogen atoms, and (3) oxygen. The compound (IV) can be prepared with safety through simple and easy operations.
摘要:
Compounds represented by the following general structural formula (1) and methods for producing the compounds: ##STR1## R.sup.1 represents a group such as benzyloxycarbonyl, R.sup.2 represents a lower alkyl group, R.sup.3 represents a hydrogen atom or a protecting group, each of M.sup.1 and M.sup.2 represents a metal atom, and n represents the atomic valence of M.sup.1. Intermediates for HMG-CoA reductase inhibitors can be prepared safely and easily from these compounds.
摘要:
A process for for producing a (2R,3S)-cyclohexylnorstatine or a salt thereof is disclosed, which comprises the steps of: enantioselectively hydrogenating a 4-cyclohexyl-2-halogeno-3-oxobutyric acid ester in the presence of a ruthenium-phosphine complex to produce a 4-cyclohexyl-2-halogeno-(3R)-hydroxybutyric acid ester (2); epoxidizing the compound (2) in the presence of a base to produce a 4-cyclohexyl-(2S,3R)-epoxybutyric acid ester (3); reacting the compound (3) with a lower trialkylsilyl azide in the presence of a Lewis acid to produce a (3S)-azide-4-cyclohexyl-(2S)-substituted butyric acid ester (4); subjecting the compound (4) to hydrogenolysis to produce a (2S,3S)-cyclohexylnorstatine derivative (5); and inverting the configuration at the 2-position of the compound (5).
摘要:
A process for preparing optically active 4-methyl-2-oxetanone which comprises asymmetrically hydrogenating 4-methylene-2-oxetanone in the presence of a ruthenium-optically active phosphine complex. Optically active 4-methyl-2-oxetanone can easily and economically be obtained at high optical purity.
摘要:
A process for preparing optically active 4-methyl-2-oxetanone which comprises asymmetrically hydrogenating 4-methylene-2-oxetanone in the presence of a ruthenium-optically active phosphine complex. Optically active 4-methyl-2-oxetanone can easily and economically be obtained at high optical purity.
摘要:
A process for producing an optically active alcohol represented by formula (I): ##STR1## wherein R.sub.1 is an alkyl group having from 2 to 11 carbon atoms, an alkenyl group having from 3 to 11 carbon atoms, an alkadienyl group having from 6 to 11 carbon atoms, a cyclohexyl group, an cyclohexylmethyl group, or a cyclohexylethyl group, provided that the olefin in the alkenyl group or alkadienyl group is not conjugated to the olefin at the 2-position thereof; and * means an asymmetric carbon atom,is disclosed, comprising subjecting an olefinic alcohol represented by formula (II): ##STR2## wherein R.sub.1 is the same as defined above to asymmetric hydrogenation in the presence of, as a catalyst, a ruthenium-optically active phosphine complex.According to the process of the invention, the desired optically active alcohols which are useful not only as intermediates for the manufacture of perfumes and vitamin E but also as liquid crystal materials can be produced with high optical purities.
摘要:
A process for preparing carnitine which comprises asymmetrically hydrogenating a .gamma.-halogeno-.beta.-keto ester represented by formula (I): ##STR1## wherein X represents a chlorine atom or a bromine atom; and R represents a lower alkyl group, in the presence of a ruthenium-optically active phosphine complex represented by formula (II), (III) or (IV):Ru.sub.2 Cl.sub.4 (L).sub.2 (C.sub.2 H.sub.5).sub.3 N (II)Ru(OCOR.sup.2).sub.2 (L) (IV)RuX.sub.2 (L) (V)wherein L represents 2,2'-bis(di-p-R.sup.1 -phenylphosphino)- 1,1'-binaphthyl of formula (III): ##STR2## wherein R.sup.1 represents a hydrogen atom, a methyl group, or a t-butyl group;R.sup.2 represents a lower alkyl group or a trifluoromethyl group; and X is as defined above,as a catalyst at a temperature of from 70.degree. to 150.degree. C. to obtain an optically active alcohol represented by formula (VI): ##STR3## wherein X and R are as defined above, and then reacting the optically active alcohol as obtained with trimethylamine without isolation, is disclosed.