59394-30-8Relevant articles and documents
Repurposing an Aldolase for the Chemoenzymatic Synthesis of Substituted Quinolines
Fansher, Douglas J.,Granger, Richard,Kaur, Satinderpal,Palmer, David R. J.
, p. 6939 - 6943 (2021/06/28)
Quinoline derivatives are important natural products and pharmaceuticals, but their synthesis can be challenging due to poor yields, harsh reaction conditions, and instability of starting materials. Here we report the chemoenzymatic synthesis of quinaldic acids under mild conditions using an aldolase, trans-o-hydroxybenzylidenepyruvate hydratase-aldolase (NahE, or HBPA). A series of 2-aminobenzaldehydes derived from reduction of the corresponding nitro analogue were reacted with pyruvate in the presence of NahE to give substituted quinolines in up to 93% isolated yield. This reaction differs from the aldol condensation catalyzed by NahE in vivo, instead resembling the heterocycle formation catalyzed by its homologue, dihydrodipicolinate synthase.
Synthesis of lodopyridone
George, Ian R.,Lewis, William,Moody, Christopher J.
, p. 8209 - 8215 (2013/09/02)
The total synthesis of the unusual 4-pyridone marine metabolite lodopyridone has been achieved by late stage manipulation of the related 4-pyrone. Key reactions include a Suzuki-Miyaura coupling to form the tetracyclic core and a modified Corey-Ganem-Gilman reaction to install the ethanolamide side-chain.
5-Sulphanyl-4h-1,2,4-triazole derivatives and their use as medicine
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Page/Page column 11, (2008/06/13)
The invention concerns novel 5-sulphanyl-4H-1,2,4-triazole derivatives of formula (1), wherein: R1, R2 and R3 represent variable groups and the methods for preparing them by liquid-phase parallel synthesis processes. Said product exhibit good affinity for certain sub-types of somatostatin receptors; they are particularly useful for treating pathological conditions or diseases wherein one (or more) somatostatin receptors is (are) involved. The invention also concerns pharmaceutical compositions containing said products and their use for preparing a medicine.