134218-80-7Relevant articles and documents
The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives
Platonova, Yana B.,Tomilova, Larisa G.,Volov, Alexander N.
, (2020)
A series of new 5-alkynyl-substituted uracil and uridine derivatives were synthesised via palladium-catalysed Sonogashira cross-coupling reaction of 5-bromo-pyrimidine base with terminal acetylenes with good yields in DMF at room temperature. All obtained compounds were tested for antimycobacterial activity against Mycobacetrium bovis and Mycobacterium tuberculosis (H37Ra) at concentrations of 1–100 μg/ml using MABA test. Obtained results revealed that most of tested uracil derivatives exhibited high antimycobacterial activity (MIC50 = 1.1–19.2 μg/ml) in comparison with therapeutic agents such as rifampicin, isoniazid and D-cycloserine, excluding compounds having alkyl substituent at triple alkyne bond.
Efficient palladium-mediated or base-induced 5-endo-dig cyclisation of C5-alkynylated pyrimidine derivatives: Conventional and microwave-assisted synthesis of novel furo[2,3-d]pyrimidines
Kraljevi?, Tatjana Gazivoda,Bistrovi?, Andrea,Dedi?, Matea,Paveli?, Sandra Kraljevi?,Sedi?, Mirela,Rai?-Mali?, Silvana
supporting information; experimental part, p. 5144 - 5147 (2012/09/25)
A series of the novel 5-alkynyl- and furo[2,3-d]pyrimidine derivatives in which the sugar moiety is replaced by a methoxymethyl (MOM) group is synthesised using the Sonogashira cross-coupling reaction under both conventional and microwave conditions, in g
Efficient solvent- and metal-free Sonogashira protocol catalysed by 1,4-diazabicyclo(2.2.2) octane (DABCO)
Luque, Rafael,MacQuarrie, Duncan J.
experimental part, p. 1627 - 1632 (2009/06/28)
An efficient metal-free Sonogashira coupling protocol catalysed by DABCO is reported, where very good conversions and selectivities to the cross-coupling product were obtained under mild reaction conditions. The reported solvent-, phosphane- and metal-free protocol, that uses a cheap base as catalyst, considerably improves the green credentials of the reaction.