PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. 1. (canceled)3. The production method according to claim 2 , wherein the dehalogenation is performed in the presence of a base.12. (canceled)16. The method according to claim 7 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof.18. The method according to claim 17 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof. The present invention relates to a production method of a pyrrole compound useful as a pharmaceutical product, particularly an acid secretion inhibitor, a production method of an intermediate used for this method, a novel intermediate and the like.A pyrrole compound having a substituted sulfonyl group at the 1-position (hereinafter to be referred to as a sulfonylpyrrole compound) is useful as an acid secretion inhibitor (proton pump inhibitor), a therapeutic drug for a neoplastic disease or an autoimmune disease (patent documents 1-3).For example, patent document 2 describes, as a compound having an acid secretion suppressive activity, a compound represented by the formula:wherein ris a monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a heterocycle, wherein the monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has ...

5-ARYL-1H-PYRROLE-3-CARBONITRILE AND A PHARMACEUTICAL PRODUCT USING THE SAME

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. 1. (canceled)3. The production method according to claim 2 , wherein the dehalogenation is performed in the presence of a base.12. (canceled)14. (canceled)16. The method according to claim 7 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof.18. The method according to claim 17 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof. The present invention relates to a production method of a pyrrole compound useful as a pharmaceutical product, particularly an acid secretion inhibitor, a production method of an intermediate used for this method, a novel intermediate and the like.A pyrrole compound having a substituted sulfonyl group at the 1-position (hereinafter to be referred to as a sulfonylpyrrole compound) is useful as an acid secretion inhibitor (proton pump inhibitor), a therapeutic drug for a neoplastic disease or an autoimmune disease (patent documents 1-3).For example, patent document 2 describes, as a compound having an acid secretion suppressive activity, a compound represented by the formula:wherein ris a monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a heterocycle, wherein the monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a heterocycle ...

Process for preparing optically active 2,3-dihydrobenzofuran compounds

A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R 1 and R 2 are each hydrogen or an optionally substituted hydrocarbon group; R 3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

ALPHA-CARBOLINE DERIVATIVES AND METHODS FOR PREPARATION THEREOF

To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously. A method for preparation of a compound represented by Formula (II) or a salt thereof, comprising subjecting a compound represented by Formula (I) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base; a method for preparation of a compound represented by Formula (IX) or a salt thereof, comprising subjecting a compound represented by Formula (VII) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base, and subsequently to an aromatization reaction; and methods for preparation of compounds represented by Formulae (XV), (XVII), and (XIX) or a salt thereof, comprising subjecting respective compounds represented by Formulae (II) and (IX) or a salt thereof to a reaction for introducing a leaving group when necessary, and subsequently to a coupling reaction: wherein ...

Highly Selective Novel Amidation Method

The present invention provides an industrial production method with a short process having a high yield of an aliphatic cyclic carboxamide having carboxyl group, which comprises reacting functional group-selectively using an inexpensive condensing agent without protecting the carboxyl group by esterification, that is, reacting carboxylic acid anhydride obtained by reacting carboxylic acid and tertiary carboxylic acid halide with aliphatic cyclic secondary amine having carboxyl group.

Process for producing pyrrole compound

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. 1. (canceled)3. The production method according to claim 2 , wherein the dehalogenation is performed in the presence of a base.4. (canceled)12. (canceled)14. (canceled)16. The method according to claim 7 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof.18. The method according to claim 17 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof. The present invention relates to a production method of a pyrrole compound useful as a pharmaceutical product, particularly an acid secretion inhibitor, a production method of an intermediate used for this method, a novel intermediate and the like.A pyrrole compound having a substituted sulfonyl group at the 1-position (hereinafter to be referred to as a sulfonylpyrrole compound) is useful as an acid secretion inhibitor (proton pump inhibitor), a therapeutic drug for a neoplastic disease or an autoimmune disease (patent documents 1-3).For example, patent document 2 describes, as a compound having an acid secretion suppressive activity, a compound represented by the formula:wherein ris a monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a heterocycle, wherein the monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a ...

Process for preparing optically active 2,3-dihydrobenzofuran compounds

A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound:[wherein R<1 >and R<2 >are each hydrogen or an optionally substituted hydrocarbon group; R<3 >is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Process for preparing optically active 2,3-dihydrobenzofuran compounds

A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Process for preparing optically active 2,3-dihydrobenzofuran compounds

A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R¹ and R² are each hydrogen or an optionally substituted hydrocarbon group; R³ is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

Agent for preventing or treating neuropathy

The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR 2 —, —CONR 2 — or —NR 2 CO— (R 2 is a hydrogen atom or an optionally substituted alkyl group); Y is a bond or a divalent acyclic hydrocarbon group; R 1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be —O—, or a salt thereof.

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. 1. (canceled)3. The production method according to claim 2 , wherein the dehalogenation is performed in the presence of a base.4. (canceled)11. (canceled)12. (canceled)14. (canceled)16. The method according to claim 7 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluoropheny1)-1-(pyridin-3-ylsulfony1)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof.18. The method according to claim 17 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluoropheny1)-1-(pyri din-3-ylsulfony1)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof. The present invention relates to a production method of a pyrrole compound useful as a pharmaceutical product, particularly an acid secretion inhibitor, a production method of an intermediate used for this method, a novel intermediate and the like.A pyrrole compound having a substituted sulfonyl group at the 1-position (hereinafter to be referred to as a sulfonylpyrrole compound) is useful as an acid secretion inhibitor (proton pump inhibitor), a therapeutic drug for a neoplastic disease or an autoimmune disease (patent documents 1-3).For example, patent document 2 describes, as a compound having an acid secretion suppressive activity, a compound represented by the formula:wherein ris a monocyclic nitrogen-containing heterocyclic group optionally condensed with a benzene ring or a heterocycle, wherein the monocyclic nitrogen-containing heterocyclic group optionally condensed with a ...

5-aryl-1H-pyrrole-3-carbonitrile and a pharmaceutical product using the same

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Agent for preventing or treating neuropathy

The present invention provides an agent for preventing or treating neuropathy having superior action and low toxicity. This agent comprises a compound represented by the formula: wherein ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent(s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is —O—, —S—, —NR 2 —, —CONR 2 — or —NR 2 CO— (R 2 is a hydrogen atom or an optionally substituted alkyl group); Y is a bond or a divalent acyclic hydrocarbon group; R 1 is an optionally substituted cyclic group, an optionally substituted amino group or an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be —O—, or a salt thereof.

PRODUCTION METHOD OF OPTICALLY ACTIVE DIHYDROBENZOFURAN DERIVATIVE

Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like. 3. The production method according to claim 1 , wherein Ris a hydroxy group.6. The production method according to claim 2 , wherein R claim 2 , R claim 2 , Rand Rare each an isopropyl group.7. The production method according to claim 1 , wherein the ruthenium complex is a complex represented by the formula:{'br': None, 'sub': 2', 'n, 'i': 'dmf', 'RuCl(L)()\u2003\u2003(V)'}wherein L is an optically active form of 1,2-bis(2,5-diisopropylphosphorano)benzene;dmf is N,N-dimethylformamide; and,n is an integer of one or more.8. The production method according to or claim 1 , wherein R claim 1 , Rand Rare each a phenyl group claim 1 ,{'sup': B4', 'B5, 'sub': '1-6', 'Rand Rare each independently a Calkyl group, and'}{'sup': 'B6', 'Ris a hydrogen atom.'}12. A ruthenium complex represented by the formula:{'br': None, 'sub': 2', 'n, 'i': 'dmf', 'RuCl(L)()\u2003\u2003(V)'}wherein L is an optically active form of 1,2-bis(2,5-diisopropylphosphorano)benzene;dmf is N,N-dimethylformamide; and,n is an integer of one or more.21. A crystal of [(3S)-6-({2′ claim 1 ,6′-dimethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2 claim 1 ,3-dihydro-1-benzofuran-3-yl]acetic acid claim 1 , showing a powder X-ray diffraction pattern having characteristic peaks at lattice spacing (d) of about 19.24±0.2 claim 1 , 18.79±0.2 claim 1 , 6.35±0.2 claim 1 , 5.37±0.2 claim 1 , 4.91±0.2 and 4.83±0.2 angstroms by powder X-ray diffraction. The present invention relates to a production method of an optically active dihydrobenzofuran derivative and the like.A compound having an optically active dihydrobenzofuran ring (e.g., [(3S)-6-({2′,6′-dimethyl-4′-[3-(methylsulfonyl)propoxy]biphenyl-3-yl}methoxy)-2,3-dihydro-1-benzofuran-3-yl]acetic acid) as ...

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction. 1. (canceled)3. The production method according to claim 2 , wherein the dehalogenation is performed in the presence of a base.16. The method according to claim 7 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof.18. The method according to claim 17 , wherein the compound represented by the formula (VIII) is 1-[5-(2-fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylmethanamine or a salt thereof. This application a continuation of U.S. patent application Ser. No. 13/203,441 filed Aug. 25, 2011. U.S. Ser. No. 13/203,441 is the national phase application pursuant to 35 U.S.C. §371 of International Application No. PCT/JP2010/052874, filed Feb. 24, 2010, which claims the benefit of priority of Japanese Patent No. 2009-042975, filed Feb. 25, 2009. These applications are hereby incorporated herein by reference in their entireties.The present invention relates to a production method of a pyrrole compound useful as a pharmaceutical product, particularly an acid secretion inhibitor, a production method of an intermediate used for this method, a novel intermediate and the like.A pyrrole compound having a substituted sulfonyl group at the 1-position (hereinafter to be referred to as a sulfonylpyrrole compound) is useful as an acid secretion inhibitor (proton pump inhibitor), a therapeutic drug for a neoplastic disease or an autoimmune disease ( ...

Process for producing pyrrole compound

Process for producing pyrrole compound

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Process for producing pyrrole compound

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Process for producing pyrrole compound

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Process for producing pyrrole compound

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Process for producing pyrrole compound

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Procedure to produce pyrrole compound

Un método de producción de un compuesto representado por la fórmula **(Ver fórmula)** en donde R1 es un grupo hidrocarbilo opcionalmente sustituido o un grupo heterocíclico opcionalmente sustituido, y R2 es un átomo de hidrógeno, un grupo alquilo opcionalmente sustituido, un grupo acilo, un grupo hidroxi opcionalmente sustituido, un grupo amino opcionalmente sustituido, un átomo de cloro o un átomo de flúor, o una sal de los mismos, que comprende someter un compuesto representado por la fórmula **(Ver fórmula)** en donde X1 es un átomo de halógeno y otros símbolos son como se han definido antes, o una de sus sales, a deshalogenación en presencia de una fuente de hidrógeno, un catalizador metálico y una baseseleccionada de una amina aromática y una amina terciaria. A method of producing a compound represented by the formula ** (See formula) ** wherein R1 is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group, and R2 is a hydrogen atom, an optionally substituted alkyl group, a acyl group, an optionally substituted hydroxy group, an optionally substituted amino group, a chlorine atom or a fluorine atom, or a salt thereof, which comprises submitting a compound represented by the formula ** (See formula) ** into where X1 is a halogen atom and other symbols are as defined above, or a salt thereof, upon dehalogenation in the presence of a hydrogen source, a metal catalyst and a selected base of an aromatic amine and a tertiary amine.

OPTIMALLY ACTIVE DIHYDROBENZOFURAN DERIVATIVE PRODUCTION METHOD

SE PROPORCIONA UN MÉTODO DE PRODUCCIÓN DE UN DERIVADO DE DEHIDROBENZOFURANO ÓPTICAMENTE ACTIVO. UN MÉTODO DE PRODUCCIÓN DE UNA FORMA ÓPTICAMENTE ACTIVA DE UN COMPUESTO REPRESENTADO POR LA FÓRMULA (X) EN DONDE CADA SÍMBOLO ES COMO SE DEFINIÓ EN LA MEMORIA DESCRIPTIVA O DE UNA DE SUSU SALES, Y SIMILARES.-

Production method of optically active dihydrobenzofuran derivative

Provided is a production method of an optically active dihydrobenzofuran derivative. A production method of an optically active form of a compound represented by the formula: wherein each symbol is as defined in the specification, or a salt thereof and the like.

AGENT FOR THE PREVENTION OR TREATMENT OF NEUROPATHIES

La presente invencion provee un agente para prevenir o tratar neuropatia que tiene una accion superior y baja toxicidad. Este agente comprende un compuesto representado por la formula: (I)

PROCESS FOR PREPARING OPTICALLY ACTIVE 2,4-DIHYDROBENZOFURAN COMPOUNDS

5-membered aromatic heterocycle derivatives as prophylactic and therapeutic agents for treating neuropathy

The present disclosure provides an agent of formula (II) for preventing or treating neuropathy having superior action and low toxicity, wherein: ring A is a 5-membered aromatic heterocycle containing 2 or more nitrogen atoms, which may further have substituent (s); B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a divalent acyclic hydrocarbon group; Z is -O-, -S-, -NR2-, -CONR2- or -NR2CO- (R2 is a hydrogen atom or an optionally substituted alkyl group); Y and Y1 are the same or different and each is a bond or a divalent acyclic hydrocarbon group; and D is a ring optionally further having substituent (s); R3 is an optionally substituted acyl group or an optionally substituted heterocyclic group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not be -O- and provided that when the 5-membered aromatic heterocycle represented by ring A is pyrazole, X is methylene, Z is -S- and Y is a bond, then the ring represented by D should not be oxadiazole, or a salt thereof.

Method for producing cyanodihydropyridine compound

【課題】非対称シアノジヒドロピリジン化合物および非対称シアノピリジン化合物の簡便な製造方法の提供。 【解決手段】式（Ｉ）〜（ＩＩ）の化合物およびＲ ４ −ＣＨＯ（ＩＩＩ）の化合物を反応させることを特徴とする、式（ＩＶ）の化合物の製造方法。 【化１】 【化２】 【化３】 ［各式中の各記号は明細書に記載の通りである。］ 【選択図】 なし

Agent for preventing or treating neuropathy

The present invention provides an agent for preventing or treating neuropath y having superior action and low toxicity. This agent comprises a compound represented by the formula:wherein ring A is a 5-membered aromatic heterocyc le containing 2 or more nitrogen atoms, which may further have substituent(s);B is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group;X is a divalent acyclic hydrocarbon group;Z is -O-, -S-, - NR2-, -CONR2- or -NR2CO- (R2 is a hydrogen atom or an optionally substituted alkyl group);Y is a bond or a divalent acyclic hydrocarbon group;R1 is an optionally substituted cyclic group, an optionally substituted amino group o r an optionally substituted acyl group, provided that when the 5-membered aromatic heterocycle represented by ring A is imidazole, then Z should not b e - O-, or a salt thereof.

Production method of optically active dihydrobenzofuran derivative

Alpha-carboline derivatives and methods for preparation thereof

To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously. A method for preparation of a compound represented by Formula (II) or a salt thereof, comprising subjecting a compound represented by Formula (I) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base; a method for preparation of a compound represented by Formula (IX) or a salt thereof, comprising subjecting a compound represented by Formula (VII) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base, and subsequently to an aromatization reaction; and methods for preparation of compounds represented by Formulae (XV), (XVII), and (XIX) or a salt thereof, comprising subjecting respective compounds represented by Formulae (II) and (IX) or a salt thereof to a reaction for introducing a leaving group when necessary, and subsequently to a coupling reaction: wherein the symbols respectively represent the same meaning as defined in the present specification.

Agent for preventing or treating neuropathy

Verfahren zur herstellung von optisch aktiven 2,4-dihydrobenzofuranverbindungen

Highly selective novel amidation method

The present invention provides an industrial production method with a short process having a high yield of an aliphatic cyclic carboxamide having carboxyl group, which comprises reacting functional group-selectively using an inexpensive condensing agent without protecting the carboxyl group by esterification, that is, reacting carboxylic acid anhydride obtained by reacting carboxylic acid and tertiary carboxylic acid halide with aliphatic cyclic secondary amine having carboxyl group.

Process for preparing optically active 2,3-dihydro- benzofuran compounds

Ny svaert selektiv amideringsmetode

Den foreliggende oppfinnelsen tilveiebringer en industriell produksjonsmetode med et hurtig prosessforløp med et høyt utbytte av alifatisk cyklisk karboksamid med karboksylgruppe, omfattende funksjonell gruppeselektiv reaksjon ved bruk av et billig kondenseringsmiddel uten å beskytte karboksylgruppen ved forestring, dvs. at det oppnådde karboksylsyreanhydridet omsettes ved å reagere karboksylsyre og tertiært karboksylsyrehalogenid med alifatisk cyklisk sekundært amin med karboksylgruppe.

Intermediates for use in a process of producing pyrrole compounds

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

Procede d'une nouvelle amidation tres selective

La présente invention divulgue un procédé industriel court de production, à rendement élevé, d'un carboxamide cyclique aliphatique ayant un groupe carboxyle, qui consiste à faire réagir sélectivement un groupe fonctionnel en utilisant un agent de condensation non coûteux sans protéger le groupe carboxyle par estérification, c'est-à-dire en faisant réagir un anhydride d'acide carboxylique, obtenu par la réaction d'un acide carboxylique et d'un halogénure d'acide carboxylique tertiaire, avec une amine secondaire cyclique aliphatique ayant un groupe carboxyle.

Metodo de amidacion novedoso altamente selectivo

La presente invencion proporciona un metodo de produccion industrial con un procedimiento corto que tiene un rendimiento elevado de una carboxamida ciclica alifatica que tiene un grupo carboxilo, el cual comprende hacer reaccionar selectivamente un grupo funcional utilizando un agente de condensacion barato sin proteger el grupo carboxilo por esterificacion, es decir, hacer reaccionar el anhidrido de acido carboxilico obtenido al hacer reaccionar acido carboxilico y haluro de acido carboxilico terciario con una amina secundaria ciclica alifatica que tiene un grupo carboxilo.