- Synthetic approach to telomerase inhibitor dictyodendrin B: Synthesis of the pyrrolo[2,3-c]carbazole core
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The core structure of the telomerase inhibitor, dictyodendrin B, was synthesized by using the palladium-catalyzed cross-coupling reaction of 3-aryl-1-(2-arylethyl)-4-hydroxy-2,5-bismethoxycarbonylpyrrole triflate with 7-alkoxyindole-3-boronate as the key step.
- Hirao, Shotaro,Sugiyama, Yumiko,Iwao, Masatomo,Ishibashi, Fumito
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scheme or table
p. 1764 - 1772
(2010/03/24)
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- Novel substituted [1,4] benzodioxino[2,3-e] isoindole derivatives, method for preparing and pharmaceutical compositions containing same
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Compounds of formula (I): wherein: A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R2 represents a hydrogen atom and in that case: R3 represents a group selected from a hydrogen atom and the groups linear or branched (C1-C6)alkyl, aryl, aryl-(C1-C6)alkyl (in which the alkyl moiety is linear or branched) and SO2CF3, or R2 and R3 form a bond, R1 represents a group selected from a hydrogen atom and the groups linear or branched (C1-C6)alkyl, aryl and aryl-(C1-C6)alkyl (in which the alkyl moiety is linear or branched) or a linear or branched (C1-C6)alkylene chain, Z1 and Z2 each represent a hydrogen atom or Z1 and Z2, together with the carbon atoms carrying them, form a phenyl group. Medicaments.
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Page/Page column 13
(2010/10/19)
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- Therapeutic diphenyl ether ligands
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This invention is directed to compounds of formula Ia, Ib or Ic and to pharmaceutical compositions thereof: or a prodrug thereof and a pharmaceutically acceptable carrier, wherein the R groups are defined in the specification; and, in which the dashed line represents an optional double bond. The invention is also directed to methods of treating, diagnosing, and preventing disorders of the central nervous system that are associated with 5HT receptors, including obesity, attention deficit disorder, migraine, depression, epilepsy, anxiety, Alzheimer's disease, withdrawal from drug abuse, pain, schizophrenia, stress-related disorders, panic disorder, sleep disorders, phobias, obsessive compulsive disorder, post-traumatic-stress syndrome, immune system depression, stress-induced gastrointestinal dysfunction, stress-induced cardiovascular dysfunction, and sexual dysfunction.
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Page/Page column 36
(2010/10/20)
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- Benzocarbapenems from indoles
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The 8,8a-dihydroazeto[1,2-a]indol-2(1H)-ones (benzocarbapenems) 1a, 16, 17, 22, 27, 35 and 36 have been prepared by cyclodehydration of the corresponding β-amino acids, these amino acids being obtained by reduction of the analogous 2-substituted or 2,7-disubstituted indoles. The hydroxy group of compound 36 is designed to mimic the carboxylic acid function of the carbapenems on the basis of molecular modelling. The azetidinones 1a and 27, which are unsubstituted at the methylene group of the four-membered ring, are unstable and highly susceptible to ring opening by nucleophiles but the compounds 22,35 and 36 with two methyl substituents at this position are much more stable. The carbonyl stretching frequency in the IR is close to 1770 cm-1 for all the azetidinones except the phenol 36 for which the absorption is at 1735 cm-1. An X-ray crystal structure of compound 36 is reported.
- Coulton, Steven,Gilchrist, Thomas L.,Graham, Keith
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p. 1193 - 1202
(2007/10/03)
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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 synthesis of 7-alkoxyindoles
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A number of protected 7-hydroxyindoles was prepared by reaction of the protected 2-nitrophenols with vinylmagnesium bromide. Benzhydryl was shown to be the protecting group of choice, giving good yields of the indole and being readily removed for subsequent transformations of the 7-hydroxy function.
- Dobson,Todd,Gilmore
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p. 611 - 617
(2007/10/02)
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