An efficient protocol for solid phase aminothiazole synthesis

Diaminothiazoles Inhibit Angiogenesis Efficiently by Suppressing Akt Phosphorylation

“…DAT1 and its analogs were synthesized through a green chemistry route that involved some process simplification of a procedure reported earlier (Sreejalekshmi et al, 2006). The details of the synthesis and characterization of the analogs will be published separately.…”

Combinatorial Chemistry Online

“…A solutionphase library approach was used to make a number of further analogues via a strategy that involved the use of crossconjugated trienes as central building blocks facilitating two consecutive cycloadditions with different dienophiles. Three naphthoquinones (2) were reacted with a range of six cross-conjugated trienes (3), and then, the Diels-Alder products reacted with a set of ten maleimides (4). Following preparative hplc, the products (5) were obtained in 27 to 86% yield, with ninety-five percent showing purities exceeding 90%.…”

“…The polymer-bound carbohydrate substrate was cleaved from the resin with different carbon nucleophiles in a cobalt-mediated Nicholas reaction. 5 A facile method for the solid-phase synthesis of pyrrolo [2,1-c] [1,4]benzodiazepine dimers has been developed. p-Nitrophenyl carbonate Wang resin attached to 2-amino-5-methoxy-methyl benzoate has been utilised as the resin-bound starting material and these reactions were monitored by FT-IR spectroscopy of resin beads.…”

“…The Groebke-type multi-component reaction (MCR) between 3-amino-1,2,4-triazole, aromatic aldehydes and isonitriles has been studied from the viewpoint of convenient generation of combinatorial arrays of imidazo [1,2-b] [1,2,4]triazoles. However, it has been established that the desired heterocyclic structures can be produced in moderate to good yields in an oxidised form, when benzylic isonitriles are used.…”

Synthesis of aminothiazoles: polymer-supported approaches

“…It was reported that the second step tracelessly removes the solid support via eliminative aromatization to afford the 2,4-diamino-5-ketothiazoles 78 (Scheme 13). 65 Although this strategy involved a solid-support protocol, the targeted products were puried by column chromatography. Reuse of the resin was found to be inefficient and it enormously affected the yield.…”