Hernandez-Vazquez, Eduardo; Miranda, Luis D. published an article in 2016, the title of the article was Practical synthesis and cytotoxic evaluation of the pyrazino[1,2-b]-isoquinoline ring system.Electric Literature of 887581-09-1 And the article contains the following content:
A practical three-step protocol for the synthesis of pyrazino[1,2-b]isoquinolines I [R1 = H, 4-Me, 5-MeO, 5-F, etc.; R2 = t-Bu, cyclohexyl, 2,6-diMeC6H3, benzyl, etc.] was reported. This approach included a one-pot parallel cyclization/cyclization parallel process followed by a non-common 6-endo Heck cyclization that transformed previously constructed Ugi adducts into diversely decorated tricyclic systems. Compounds bearing a t-Bu or 2,6-dimethylphenyl substituent showed significant cytotoxic activity. The most active analog I (R1 = CH2O2; R2 = 2,6-diMeC6H3) showed significant activity against HCT-15 and K562 (IC50 = 41.8 ± 3.3 and 57.7 ± 2.1 μM, resp.) with no cytotoxicity against human gingival fibroblasts. The experimental process involved the reaction of (2-Bromo-5-methoxyphenyl)methanamine(cas: 887581-09-1).Electric Literature of 887581-09-1
The Article related to benzylamine isocyanide benzoyloxy acetaldehyde chloroacetic acid ugi reaction, bromo chloroacetylamiono oxopropylamino benzoate preparation heck reaction, pyrazinoisoquinoline preparation antitumor activity structure activity relationship and other aspects.Electric Literature of 887581-09-1
Referemce:
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Ether | (C2H5)2O – PubChem