63486-71-5Relevant articles and documents
Regiocontrol in the 1,3-dipolar cycloaddition reactions of mesoionic compounds with acetylenic dipolarophiles
Coppola, Brian P.,Noe, Mark C.,Hong, Sam Shih-Kuang
, p. 7159 - 7162 (1997)
The regioselectivity of 1,3-dipolar cycloaddition reactions between mesoionic compounds with singly-tethered substitents is examined. The results with propiolate dipolarophiles are compared with other singly and doubly-tethered examples according to a model using an asynchronous, concerted transition state. The isolation and reaction of a novel, non-aryl substituted mesoionic compound 7 is reported. A regiodirected synthesis starting with N-(2-thiazolinyl)proline gives a complementary dihydropyrroline compared with the reaction between N-formylproline and alkyl propiolates.
MCL-1 INHIBITORS
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Paragraph 0672-0673, (2019/12/01)
The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.
Synthesis and antiinflammatory and analgesic activity of 5-aroyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and related compounds
Muchowski,Unger,Ackrell,Cheung,Cooper,Cook,Gallegra,Halpern,Koehler,Kluge
, p. 1037 - 1049 (2007/10/02)
5-Acyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids and the homologous pyridine and azepine derivatives were synthesized and assayed for antiinflammatory and analgesic activity. 5-Benzoyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acid and the corresponding p-methoxy compound were selected for evaluation as analgesic agents in humans on the basis of their high potency in the mouse phenylquinone writhing assay as well as on their minimal liability to elicit gastrointestinal erosion in rats on chronic administration. Extensive quantitative structure-activity relationship (QSAR) studies of the benzoylpyrrolopyrrolecarboxylic acids have demonstrated that the analgesic (mouse writhing) and antiinflammatory (rat carrageenan paw) potencies of these compounds are satisfactorily correlated with the steric and hydrogen-bonding properties of the benzoyl substituent(s). The 4-vinylbenzoyl compound, which was correctly predicted to be highly active in both assays on this basis, is undergoing advanced pharmacological evaluation in animals as a potential antiinflammatory agent.