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JP5192856B2 |
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JP5193664B2 |
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JP5192370B2 |
SUMMARY OF THE INVENTION The invention relates to a method for preparing a sulphoxide compound of formula (I) either as a single enantiomer or in an enantiomerically enriched form, comprising the steps of: a) contacting a pro-chiral sulp...
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JP5191385B2 |
The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic aci...
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JP5192541B2 |
The invention concerns a new process for the preparation of naphthoquinones, in particular an improved process for the preparation of 2,3-disubstituted 1,4-naphthoquinones, in the trans configuration.
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JP2013079249A |
To provide a method for the conversion of oximes that can be obtained easily without using a metallic reagent, to corresponding enamides in good yield.A method of producing enamides shown by the following formula 3 and the like, which un...
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JP5186722B2 |
It was found that a fluoro derivative can be produced by reacting a hydroxy derivative with sulfuryl fluoride (SO 2 F 2 ) in the presence of an organic base or in the presence of an organic base and "a salt or complex comprising an organ...
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JP5184783B2 |
Process for the preparation of tetrahydrobiopterin from neopterin and/or 6-substituted pterins with an improved yield and a high stereoselectivity. Also disclosed herein are novel individual intermediates prepared in the preparation of t...
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JP5185485B2 |
Compounds of the formula (I) and (Ia) in the form of racemates, mixtures of diastereomers or in essentially enantiomerically pure form, (I), (Ia), where R is hydrogen, C1-C8alkyl, C5-C12cycloakyl, phenyl or phenyl substituted by from 1 t...
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JP5178989B2 |
The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, methods for the...
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JP5179430B2 |
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JP5178052B2 |
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JP5179546B2 |
The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; and n is an integer from 10 to 18 or a pharmaceutically acceptable derivative thereof, methods for the...
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JP5180289B2 |
The present invention relates to a process for preparing (3R,4S)-3-[[[R]-V-t- butyldimethylsilyloxy] ethyl] -4- [(/?)- l"-carboxyethyl]-2-azetidinone [4-BMA: formula (6)], a key intermediate for the synthesis of carbapenem and penem anti...
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JP5180596B2 |
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JP5180965B2 |
Preparation of N-[3-[(2-methoxyphenyl)sulfanyl]-2-methylpropyl]-3,4-dihydro
-2H-1,5-benzoxathiepin-3-amine (I) comprises condensation of 7,8-dihydro-6H-5-oxa-9-thia-benzocyclohepten-7-ylamine compound (II) and 5-methoxy-6-(2-methyl-butyl...
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JP5173775B2 |
The present invention relates to a novel process for producing a delta -lactone of the formula: using an acyl halide of the formula: wherein R<1>, R<2> R<3> and X are described herein, as well as novel intermediates. In particular, the p...
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JP2013510891A |
This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives.
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JP5170382B2 |
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JP5172124B2 |
The invention provides a method for producing optically active 3-quinuclidinols having one or more substituted groups at the 2-position; wherein 3-quinuclidinones having one or more substituted groups at the 2-position are reacted with c...
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JP5167130B2 |
This invention provides a method for making maytansinoids having a chiral amino acid side chain, such as DM1 and DM4 that are used to treat cancer. According to this method, the side chain may be added with little epimerization of the am...
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JP5166029B2 |
Provide that a useful catalyst for homogeneous hydrogenation, particularly a catalyst for homogeneous asymmetric hydrogenation for hydrogenation, particularly asymmetric hydrogenation, which is obtainable with comparative case and is exc...
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JP2013046572A |
To provide an efficient industrial production method of an optically active 2-hydroxycycloalkanecarboxylic acid ester useful as an intermediate for a pharmaceutical product.The optically active 2-hydroxycycloalkanecarboxylic acid ester i...
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JP2013508355A |
Disclosed are a novel, simple and low-cost method for preparing sitagliptin of formula (I), as DPP-IV (dipeptidyl peptidase IV) inhibitor, which is useful in treating type 2 diabetes mellitus and key intermediates used in said preparatio...
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JP5158926B2 |
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JP5157154B2 |
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JP5159314B2 |
Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates a...
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JP5154402B2 |
An industrially advantageous process for the production of (3R,4S)-3-cyclopropylaminomethyl-4-fluoropyrrolidine or an enantiomer thereof that is useful as an intermediate for the production of novel antimicrobial agents 10-(3-cyclopropyl...
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JP5153631B2 |
The objective of the present invention is to provide an optically active imidazolidinone derivative widely usable for synthesizing an optically active amino acid, a method of easily producing the derivative, and a method of easily produc...
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JP2013035816A |
To develop a manufacturing method capable of simply synthesizing a quaternary α-trifluoromethyl ketone derivative in a high yield.The manufacturing method comprises subjecting an α-trifluoromethyl-β-ketoester to allylation reaction wi...
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JP2013035809A |
To provide optically active α-hydroxyketones useful as intermediates for medicine, agricultural chemicals, perfumes, etc.Optically active α-hydroxyketones are produced with a high yield and a high enantio-selectivity by an asymmetric c...
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JP5149238B2 |
A processes which is industrially advantageous in producing antibacterial agents. An industrially advantageous process for producing an intermediate useful in producing antibactrial agents is provided by producing compound (VI-a) in acco...
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JP2013505215A |
The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I), and also to their method of synthesis and to their use in pharmaceutical compositions intended for use i...
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JP5142716B2 |
Methods for the synthesis of cyclic phosphonic acid diesters from 1,3-diols are described, whereby cyclic phosphonic acid diesters are produced by reacting a chiral 1,3-diol and an activated phosphonic acid in the presence of a Lewis acid.
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JP5144865B2 |
Compounds of formulae I and Ia, wherein X1 is secondary phosphino; R3 is hydrogen, a hydrocarbon radical having from 1 to 20 carbon atoms, a heterohydrocarbon radical, bonded via a carbon atom, having from 2 to 20 atoms and at least one ...
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JP5137819B2 |
Method for the preparation of asymmetric alkynylated alpha-amino esters of the formula wherein R1 and R2 are independently optionally substituted alkyl cycloalkyl, aryl or heteroaryl, and Y is hydrogen or a nitrogen protecting group.
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JP5135264B2 |
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JP5139348B2 |
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JP5140673B2 |
The present invention relates to a method of working up an aluminum-containing reaction product from the production of isopulegol by cyclization of citronellal in the presence of complex compounds, comprising at least one ligand of the f...
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JP5137284B2 |
The process for obtaining 4-(N-alkylamino)-5,6-dihydro-4H-thien-(2,3-b)-thiopyran-2-su
lfonamide- 7,7-dioxides (I) wherein R1 is H or C1-5 alkyl, and R2 is C1-5 alkyl, starts from the corresponding 4-(N-alkylamino)-5,6-dihydro-4H-thien-(...
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JP5134883B2 |
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JP5130212B2 |
The present invention is a process for preparing (3R)-2′-(4-bromo-2-fluorobenzyl)spiro-[pyrrolidine-3,4′(
1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2H′)-tetraone
, comprising, for example, the following steps: (1) reacting a com...
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JP5134834B2 |
To produce a 5,5-disubstituted-3-pyrrolin-2-one derivative and an α,α-disubstituted-α-amino acid derivative useful as synthetic intermediates simply and economically. The 5,5-disubstituted-3-pyrrolin-2-one derivative is produced by re...
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JP5124950B2 |
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JP5128282B2 |
The present invention relates to a process for preparing optically active carbonyl compounds by asymmetrically hydrogenating alpha,beta-unsaturated carbonyl compounds in the presence of optically active transition metal catalysts which a...
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JP5127156B2 |
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JP5128281B2 |
The present invention is concerned with an improved method of producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide) comprising the O-methylation of a compound of formula I to produce a compound of formula II in a single s...
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JP5128126B2 |
Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmac...
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JP5127228B2 |
An industrial process for production of high-purity optically active amine derivatives in high yield while inhibiting the formation of by-products, which comprises subjecting (E)-2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-ylidene)et
h...
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JP5126540B2 |
[PROBLEMS] To provide an efficient process for producing an optically active chromene oxide compound which is an important intermediate for a benzopyran compound effective in the treatment of arrhythmia. [MEANS FOR SOLVING PROBLEMS] The ...
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