- Sulfonamide peri-substituted bicyclics for occlusive artery disease
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Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
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Page/Page column 43
(2008/06/13)
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- CARBOXYLIC ACID PERI - SUBSTITUTED BICYCLICS FOR OCCLUSIVE ARTERY DISEASE
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Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.
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Page/Page column 78; 106-107
(2010/11/08)
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- Simple synthesis of 7-formyl-indole
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A simple route to 7-formyl-indole (5) is described in which appropriately functionalized o-nitrotoluenes (1) are converted to 7-hydroxymethyl-indole (4) using the Batcho-Leimgruber process. Condensation of 3-methyl-2-nitrobenzyl alcohol (1a) with N,N-dimethylformamide dimethyl acetal yields the enamine 2a, which upon catalytic hydrogenation affords 4 in 22% yield. When the hydroxyl function in 1 is protected with pivaloyl or tetrahydropyranyl group, the yields of 4 are increased to 39% and 48%, respectively. Finally, 4 is oxidized with pyridinium chlorochromate (PCC) to afford 5 in 86% yield. Copyright Taylor & Francis Group, LLC.
- Uchil, Vinod R.,Gund, Machhindra,Satyam, Apparao
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p. 1051 - 1056
(2007/10/03)
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- N-benzyl dihydroindole LTD4 antagonists
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This invention relates to pharmaceutical N-benzyl dihydroindole compounds having the general formula: STR1 and their use as LTD4 antagonists.
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- Certain indole derivatives useful as leukotriene antagonists
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A compound of the formula STR1 in which R1 is hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C1-4 alkyl, aldehydo, --CH2 Z, --CH=CH--Z or --CH2 CH2 Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R2 is halo, nitrile, an optionally protected acid group or --CONR7 R8 where R7 and R8 are each hydrogen or C1-4 alkyl; R3 and R4 are each hydrogen, C1-4 alkyl, optionally substituted phenyl, or C1-4 alkyl substituted by --CONR7 R8 or an optionally protected acid group; R5 is STR2 where W is --CH=CH--, --CH=N--, --N=CH--, --O-- or --S--, R9 is hydrogen, halo, C1-4 alkyl, C1-4 alkoxy or trihalomethyl, and R10 is hydrogen, C1-4 alkyl, C2-6 alkenyl, C3-6 cycloalkyl or C1-4 alkyl-C3-6 cycloalkyl; R6 is hydrogen or C1-4 alkyl; X is --O--(CH2)n CR11 R12, --CR11 R12 --, --CR11 R12.(CH2)n.CR13 R14 -- or --CR11 =CR12 -- where R11, R12, R13 and R14 are each hydrogen or C1-4 alkyl, and n is 0, 1 or 2; and Y is --O--CR15 R16 --, --CR15 =CR16 -- or --CR15 R16.CR17 R18 -- where R15, R16, R17 and R18 are each hydrogen or C 1-4 alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.
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- N-Benzyl-Indoles, processes for their preparation and pharmaceutical compositions containing them
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A compound of the formula in which R1 is hydrogen, halo, C??? alkyl, C??? alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C??? alkyl, aldehydo,-CH?Z,-CH=CH-Z or-CH?CH?Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R2 is halo, nitrile, an optionally protected acid group or-CONR?R? where R? and R? are each hydrogen or C??? alkyl, R3 and R? are each hydrogen, C??? alkyl, optionally substituted phenyl, or C??? alkyl substituted by-CONR?R? or an optionally protected acid group; R? is where W is-CH=CH-,-CH=N-,-N=CH-,-O-or-S-, R? is hydrogen, halo, C??? alkyl, C? ?? alkoxy or trihalomethyl, and R1? is hydrogen, C? ?? alkyl, C??? alkenyl, C??? cycloalkyl or C??? alkyl-C??? cycloalkyl; R? is hydrogen or C??? alkyl; X is-O-(CH?)nCR11CR12-,-CR11R12-,-CR11R12.(CH?) n.CR13R1?-or-CR11=CR12-where R11, R12, R13 and R1? are each hydrogen or C??? alkyl, and n is 0, 1 or 2; and Y is-O-CR1?R1?-,-CR1?=CR1?-or-CR1? R1?.CR1?R1?-where R1?, R1?, R1? and R1? are each hydrogen or C??? alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.
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- The Chemistry of Indoles. XXXIII. Substituent Effect in Regioselective Metalation of 3-Indolecarbaldehyde and Syntheses of Indoles Carrying a Carbon Side Chain at the 4-, 5-, 6-, or 7-Position
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The nature of a substituent on the pyrrole ring of 3-indolecarbaldehyde plays a significant role in governing the regioselectivity of metalation.To confirm the structures of the products, various indoles carrying a carbon side chain at the 4-, 5-, 6-, or 7-position were prepared by other methods.Synthesis of 5-substituted 1-hydroxyindoles is also described.Keywords-thallation; mercuration; 4-substituted indole; 5-substituted indole; 6-substituted indole; 7-substituted indole; regioselective metalation; 3-indolecarbaldehyde; thallation-palladation; 1-hydroxyindole
- Somei, Masanori,Saida, Yoshihiro,Komura, Naoko
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p. 4116 - 4125
(2007/10/02)
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- Nickel(II) Complexes of Imine Ligands derived from 7-Formylindoles
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Quadridentate bis-imine nickel(II) complexes have been formed from 7-formylindoles and 1,2-diaminobenzene: an X-ray crystal structure determination of the chloroform solvate of the N,N'-bis(4,6-dimethoxyindol-7-ylidene)-1,2-diaminobenzene complex shows severe distortion from planarity and a distance of 2.96 Angstroem between the C-2 indole atoms.
- Black, David St C.,Craig, Donald C.,Kumar, Naresh,Wong, Laurence C. H.
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p. 1172 - 1173
(2007/10/02)
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