- Competitive ortho metalation effects: The kinetic and thermodynamic lithiation of 3-(tert-butoxycarbonyl)amino-4-carbomethoxythiophene
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Deprotanation of the thiophene 1 under kinetically controlled conditions with LDA takes place next to the NHBoc group and under thermodynamic conditions next to the methyl eater. N-Methylation leads to exclusive lithiation next to the ester. The methylester was found to be superior to the diethylamide in facilitating lithiation.
- Carroll, William A.,Zhang, Xiaolin
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Read Online
- Heterocyclically substituted benzimidazoles, the production and application thereof
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The present invention relates to novel benzimidazoles, their preparation and their use as inhibitors of the enzyme poly(ADP-ribose) polymerase or PARP (EC 2.4.2.30) for producing drugs.
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Page column 18-19
(2010/02/05)
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- SUBSTITUTED QUINAZOLINE DERIVATIVES AND THEIR USE AS INHIBITORS
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The use of a compound of formula (I) 1 or a salt, ester or amide thereof; where X is O, or S, S(O) or S(O)2, or NR6 where R6 is hydrogen or C1-6 alkyl,; R5 is an optionally substituted 5-membered heteroaromatic ring, R1, R2 ,R3, R4 are independently selected from various specified moieties, in the preparation of a medicament for use in the inhibition of aurora 2 kinase. Certain compounds are novel and these, together with pharmaceutical compositions containing them are also described and claimed
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- Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents
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Heterocyclic analogues of 1192U90, 2-amino-N-(4-(4-(1,2-benzisothiazol- 3-yl)-1-piperazinyl)-butyl)benzamide hydrochloride (1), were prepared and evaluated as potential antipsychotic agents. These analogues were evaluated in vitro for their binding to the dopamine D2, serotonin 5-HT2, and serotonin 5-HT(1a) receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. Nine different types of heterocyclic carboxamides were studied in this investigation (i.e., pyridine- , thiophene-, benzothiophene-, quinoline-, 1,2,3,4-tetrahydroquinoline-, 2,3- dihydroindole-, indole-, benzimidazole-, and indazolecarbox-amides). Two derivatives exhibited potent in vivo activities comparable to 1: 3-amino-N- (4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2-pyridinecarboxamide (16) and 3-amino-N-(4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2- thiophenecarboxamide (29). Furthermore, these derivatives were found to be much less active in behavioral models predictive of extrapyramidal side effects than in the mouse climbing assay, which predicts antipsychotic activity. Carboxamides 16 and 29 were selected for further evaluation as potential backup compounds to 1.
- Norman, Mark H.,Navas III, Frank,Thompson, James B.,Rigdon, Greg C.
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p. 4692 - 4703
(2007/10/03)
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- Synthesis of Thiophenedicarbonyldiazides and Di-t-butyl Thiophendicarbamates
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Dicarbamates 1b and 1c, and dicarbonyldiazides 2b and 2c are obtained in good yields starting from thiophenedicarboxylic acids 3b and 3c, but the vicinal diacids 3a and 3d are not suitable for the synthesis of dicarbamates 1a and 1d and dicarbonyldiazides 2a and 2d; 1a is prepared by a stepway procedure previously described, and 1d by t-butoxycarbonylation of the recently known 3,4-thiophenediamine.
- Galvez, Carmen,Garcia, Francisco,Garcia, Juan,Soldevila, Joan
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p. 1103 - 1108
(2007/10/02)
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