- Cyclic Anti-Azacarboxylation of 2-Alkynylanilines with Carbon Dioxide
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Direct anti-azacarboxylation of 2-alkynylanilines with CO2 mediated by ZnEt2 was observed to afford indole-3-carboxylic acids, a class of important compounds for the synthesis of many biologically active compounds, efficiently under 1 atm of CO2. The readily available nature of the different starting materials and tolerance of various functional groups provide vast opportunities for the efficient construction of diversified libraries for bioactive compounds listed in Figure 1. As an example, this methodology has been applied to the synthesis of Lotronex, a drug molecule used for the treatment of irritable bowel syndrome.
- Miao, Bukeyan,Li, Suhua,Li, Gen,Ma, Shengming
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p. 2556 - 2559
(2016/07/06)
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- PROCESS FOR THE PREPARATION OF ALOSETRON
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The present invention provides an improved process for the preparation of Alosetron of formula (I) and its pharmaceutically acceptable salts.
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Page/Page column 3
(2012/07/27)
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- INDOLONE MODULATORS OF 5-HT3 RECEPTOR
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The present invention relates to new indolone modulators of 5-HT3 receptor, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 13
(2010/05/13)
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- Medicaments
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The invention relates to the use of compounds of the general formula (I) STR1 and physiologically acceptable salts and solvates thereof, in which Im represents an imidazolyl group of formula: STR2 and R1 represents a hydrogen atom or a group selected from C1-6 alkyl, C3-6 alkenyl, C3-10 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkylC1-4 alkyl, phenyl, phenylC1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO2 R5, --COR5, --CONR5 R6 or --SO2 R5 (wherein R5 and R6, which may be the same or different each represents a hydrogen atom, a C1-6 alkyl or C3-7 cycloalkyl group, or a phenyl or phenylC1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C1-4 alkyl, C1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R5 does not represent a hydrogen atom when R1 represents a group --CO2 R5 or --SO2 R5); one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, phenyl or phenylC1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6 alkyl group; and n represents 2 or 3, for the treatment of a condition involving excessive eating, for example bulimia.
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- Medicaments
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The invention relates to the use of compounds of formula (I) STR1 wherein Im represents an imidazolyl group of formula: STR2 and R1 represents a hydrogen atom or a group selected from C1-6 alkyl, C3-6 alkenyl, C3-10 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkylC1-4 alkyl, phenyl, phenylC1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO2 R5, --COR5, --CONR5 R6 or --SO2 R5 (wherein R5 and R6, which may be the same or different, each represents a hydrogen atom, a C1-6 alkyl or C3-7 cycloalkyl group, or a phenyl or phenylC1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C1-4 alkyl, C1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R5 does not represent a hydrogen atom when R1 represents a group --CO2 R5 or --SO2 R5); one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, phenyl or phenylC1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6 alkyl group; and n represents 2 or 3, and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of depression.
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- Medicaments
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The invention relates to the use of compounds of formula (I) STR1 wherein Im represents an imidazolyl group of formula: STR2 and R1 represents a hydrogen atom or a group selected from C1-6 alkyl, C3-6 alkenyl, C3-10 alkynyl, C3-7 cycloalkyl, C3-7 cycloalkylC1-4 alkyl, phenyl, phenylC1-3 alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, --CO2 R5, --COR5, --CONR5 R6 or --SO2 R5 (wherein R5 and R6, which may be the same or different, each represents a hydrogen atom, a C1-6 alkyl or C3-7 cycloalkyl group, or a phenyl or phenylC1-4 alkyl group, in which the phenyl group is optionally substituted by one or more C1-4 alkyl, C1-4 alkoxy or hydroxy groups or halogen atoms, with the proviso that R5 does not represent a hydrogen atom when R1 represents a group --CO2 R5 or --SO2 R5); one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, phenyl or phenylC1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6 alkyl group; and n represents 2 or 3, and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of a cognitive disorder.
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- PROCESS FOR THE PREPARATION OF LACTAM DERIVATIVES
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The invention relates to a process for the preparation of a compound of formula (I) STR1 wherein R represent a hydrogen atom or a methyl or ethyl group, which comprises cyclising a compound of formul (IV) STR2 Where R represents a hydrogen atom, the compound of formula (IV) may optionally be alkylated to produce a compound in whcich R is methyl or ethyl.The compound of formula (I) is useful as an intermediate in the preparation of 2,3,4,5-tetrahydro-2-[(imidazol-4(or 5)-yl)methyl]-1H-pyrido[4,3-b]indol-1-ones having 5-HT 3 antagonist activity.
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- Use of serotonin antagonists in the treatment of cognitive disorders
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The invention relates to the use of compounds of formula wherein Im represents an imidazolyl group of formula: and R1 represents a hydrogen atom or a group selected from C1 6alkyl, C3 6alkenyl, C3 10alkynyl, C3 7cycloalkyl,C3 7cycloalkylC1 4alkyl, phenyl, phenylC1 3alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO2R5, -COR5, -CONR5R6 or -SO2R5 (wherein R5 and R6, which may be the same or different, each represents a hydrogen atom, a C1 6alkyl or C3 7cycloalkyl group, or a phenyl or phenylC1 4alkyl group, in which the phenyl group is optionally substituted by one or more C1 4alkyl, C1 4alkoxy or hydroxy groups or halogen atoms, with the proviso that R5 does not represent a hydrogen atom when R1 represents a group -CO2R5 or -SO2R5);, one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1 6alkyl, C3 7cycloalkyl, C3 6alkenyl, phenyl or phenylC1 3alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1 6 alkyl group;, and n represents 2 or 3,and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the treatment of a cognitive disorder.
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- Use of serotonin antagonists in the treatment of drug addiction.
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The invention relates to the use of compounds of formula (I)*(formula 01)* wherein Im represents an imidazolyl group of formula:*(formula 02)* and R1 represents a hydrogen atom or a group selected from C1-6alkyl, C3-6alkenyl, C3-10alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, phenylC1-3alkyl, phenylmethoxymethyl, phenoxyethyl, phenoxymethyl, -CO2R5, -COR5, -CONR5R6 or -SO2R5 (wherein R5 and R6, which may be the same or different, each represents a hydrogen atom, a C1-6alkyl or C3-7cycloalkyl group, or a phenyl or phenylC1-4alkyl group, in which the phenyl group is optionally substituted by one or more C1-4alkyl, C1-4alkoxy or hydroxy groups or halogen atoms, with the proviso that R5 does not represent a hydrogen atom when R1 represents a group -CO2R5 or -SO2R5); one of the groups represented by R2, R3 and R4 is a hydrogen atom or a C1-6alkyl, C3-7cycloalkyl, C3-6alkenyl, phenyl or phenyl C1-3alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C1-6 alkyl group; and n represents 2 or 3, and physiologically acceptable salts and solvates thereof for the manufacture of a medicament for the relief or prevention of a withdrawal syndrome resulting from addiction to a drug of substance of abuse and/or for the suppression of dependence on drugs or substances of abuse.
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