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JP2012144471A |
To provide asymmetric phosphonite compound used for a catalyst ligand or the like of axially asymmetric biaryl synthesis excellent in reactivity, turn over number, and asymmetric yield.There are disclosed an asymmetric phosphonite compou...
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JP4990427B2 |
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JP2012140390A |
To provide a method for industrially producing an α-amino-γ-butyrolactone or a salt thereof with a short reaction time, with high yield, and with excellent operability, especially to provide the method for industrially producing the α...
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JP4986847B2 |
A process for the stereoselective preparation of a P-chiral four-co-ordinated phosphorus compound, the process comprising reacting a first reactant selected from the group consisting of a chiral alcohol, chiral amine or chiral thiol, wit...
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JP4987197B2 |
To provide a method for efficiently producing an optically active trihaloanilino derivative useful for the production of an antimicrobial compound by an asymmetric reduction, and further to provide an optically active phosphine ligand us...
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JP4982917B2 |
The present invention provides a simplified and convenient process for the preparation of an optically active enone such as 7,7-dimethyl-6,8-dioxabicyclo-[3,3,0]oct-3-en-2-one.The invention further provides novel optically active interme...
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JP2012136480A |
To provide a new optically active macrocyclic compound capable of identifying asymmetry of an asymmetric compound, especially, capable of identifying asymmetry of an asymmetric compound incapable of hydrogen-bonding, to provide a product...
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JP4979590B2 |
The invention relates to compounds of the formula I wherein R, R1, R2, R3, X, and n are defined in the specification. The invention also provides pharmaceutically suitable acid addition salts thereof and all forms of optically pure enant...
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JP4979889B2 |
R-Bambuterol, being the R-enantiomer of bambuterol of the following structure and is therapeutically acceptable salts.
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JP2012515755A |
A caged phosphine product is provided which can act as a ligand to form a metal complex. The metal complex can be used as a catalyst. The caged phosphine is a compound of formula (I): or a salt thereof; wherein the groups R1 and R8 each ...
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JP4971169B2 |
The invention relates to a process for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel ( I ) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. The invention als...
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JP4969767B2 |
The present invention relates to a process for the production of compound A comprising reacting compound B with compound C. A further ring closure reaction may be necessary. The invention further relates to certain novel compounds of for...
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JP4965680B2 |
The present invention relates to a method for the deracemisation or chiral inversion of chiral amines by enzymatic treatment. The method employs a stereoselective enzymatic conversion and either a non-selective or partially selective che...
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JP4970249B2 |
Disclosed is a method for efficiently and highly selectively producing L-2-amino-4-(hydroxymethylphosphinyl)-butanoic acid, which is useful as a herbicide, through a catalytic asymmetric synthesis reaction. Specifically disclosed is a me...
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JP4966183B2 |
Materials and methods for preparing (S)-(+)-3-aminomethyl-5-methyl-hexanoic acid and structurally related compounds via enzymatic kinetic resolution are disclosed.
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JP4965256B2 |
A process for producing optically pure R-hydroxyphenoxypropanoic acid or a salt or ester thereof by reaction of hydroquinone or a salt thereof with an S-halopropanoic acid or a salt thereof in the presence of a mild reducing agent.
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JP4961562B2 |
Disclosed is a 19-norvitamin D derivative which has enhanced pharmacological effects compared with a 1,25-(OH)2D3 derivative and is not accompanied by an adverse side effect of causing hypercalcemia. Also disclosed is a process for produ...
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JP4961357B2 |
The present invention relates to an isoxazoline derivative having the cyclic carboxylic acid hemiketal moiety of formula (1) for use as caspase inhibitor, a process for preparing it, and a pharmaceutical composition comprising it.
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JP4962924B2 |
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JP4961568B2 |
Disclosed is a novel asymmetric ligand which can be synthesized by a short process at low cost and is capable of exhibiting higher catalytic activity and enantioselectivity than the conventional ligands derived from sugars. Also disclose...
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JP4963049B2 |
Disclosed is a process for producing an optically active phosphorus compound having an R- or S-type absolute configuration on phosphorus in a simple manner and at high efficiency, while avoiding racemization. An optically active phosphor...
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JP2012513966A |
A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmet...
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JP4958374B2 |
Catalyst for the asymmetric (transfer) hydrogenation represented by the formula MLaXbSc, where M is a transition metal, to be chosen from rhodium and ruthenium, and X is a counter ion and S is a ligand, a ranges from 0.5 to 3 and b and c...
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JP4958513B2 |
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JP4954886B2 |
The present invention relates to a method for preparation of substituted phenyl carbamate and pharmaceutically acceptable salts thereof, which are of current pharmaceutical interest. The substituted phenyl carbamate and pharmaceutically ...
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JP2012513445A |
Chiral compounds of the formula (1), which are optically pure or highly optically enriched in which R 0 is C 1 -C 12 -alkyl which is unsubstituted or substituted by 1 to 2 C 1 -C 4 -alkoxy; cyclopentyl or cyclohexyl, which is unsubstitut...
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JP4954378B2 |
The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula starting from furan. 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.
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JP4954201B2 |
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JP4949582B2 |
Substituted 4-phenyl-2-aminothiazole derivatives, processes for preparing the same, and the use thereof as corticotrophin releasing factor (CRF) antagonists.
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JP4950896B2 |
Compounds of formula I in salt or zwitterionic form wherein R 1 , R 2 , R 3 and R 4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially infla...
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JP2012106998A |
To provide a novel process for producing an optically active β-amino aldehyde compound from an imine compound.A process for producing an optically active β-amino aldehyde compound (3) is provided, which includes a step of making an imi...
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JP4945823B2 |
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JP4947866B2 |
Chiral ligands and transition metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The chiral ligands include chiral C1-C6 TunaPhos ligands. The ruthenium TunaPhos complex reduces ketones to the corr...
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JP4948172B2 |
One aspect of the present invention relates to cinchona-alkaloid-based catalysts. A second aspect of the invention relates to a method of preparing a derivatized cinchona-alkaloid catalyst. Another aspect of the present invention relates...
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JP2012512136A |
To provide a process for increasing the proportion of an optical isomer of not only a compound having a closed ring but also a compound not having a closed ring when an optical isomer mixture of a compound having both a formyl group and ...
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JP2012512221A |
The invention relates to a novel process for the preparation of (3S,4S)- or (3R,4R)-1-benzyl-4-(halogen-aryl)-pyrrolidine-3-carboxylic acids of formula I or salts thereof, wherein X and Y are each independently hydrogen or a halogen atom...
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JP2012102032A |
To provide a purification method capable of obtaining optically active 1,1,1-trifluoro-2-propanol with high purity.The optically active 1,1,1-trifluoro-2-propanol with high purity can be obtained by reacting with an aralkyl halide a mixt...
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JP4944012B2 |
The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5...
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JP4939679B2 |
New ionic compounds corresponding to the formula (R1X1(=Z1)Q-X2(=Z2)R2)m Mm (I) :- M = a proton or metallic cation of valence m chosen from alkali, alkaline earth, transition, rare earth metals or an organic onium cation or organo-metall...
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JP4944136B2 |
The present invention relates to a process for the efficient preparation of highly optical pure chiral carvedilol. According to the present invention, a chiral oxazolidin-2-one or oxazolidin-2-thione having formula 2, produced from the r...
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JP4943185B2 |
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JP2012097058A |
To efficiently produce carnosol and its derivative which is one of the main antioxidant active substances of lamiaceous herbs such as rosemary and sage, by using a tree ingredient of Chamaecyparis pisifera and the like as a raw material....
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JP4932707B2 |
Disclosed is a method for producing an optically active 3-methylcyclopentadecan-1-one which is characterized in that 2-cyclopentadecen-1-one is subjected to a 1,4-conjugate addition reaction of a methyl group by using a methylated organi...
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JP4930951B2 |
The present invention provides a process comprising substitution of an acceptor molecule comprising a group -XC(O)- wherein X is O, S or NR 8 , where R 8 is C 1-6 alkyl, C 6-12 aryl or hydrogen, with a nucleophile, wherein the acceptor m...
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JP4933743B2 |
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JP4926043B2 |
The present invention provides bipyrimidinyl diphosphine compounds of the formula wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R′ and R″ are independently optionally substituted alkyl, cycloalkyl, aryl o...
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JP4927563B2 |
Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acylo...
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JP4929938B2 |
A method of producing optically active ±-amino acid benzyl esters comprising reacting an optically active ±-amino acid and benzyl alcohols in the presence of an acid, wherein the reaction is carried out under reduced pressure without s...
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JP4928941B2 |
The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and their use as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
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JP4929402B2 |
By intramolecular condensation reaction of 2,15-hexadecanedione in a gaseous phase with a compound of a Group II element of the Periodic Table as a catalyst, 3-methyl-cyclopentadecenones is generated. Magnesium oxide, calcium oxide, or z...
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