96564-48-6Relevant articles and documents
Continuous flow thermolysis of azidoacrylates for the synthesis of heterocycles and pharmaceutical intermediates
O'Brien, Alexander G.,Levesque, Francois,Seeberger, Peter H.
supporting information; experimental part, p. 2688 - 2690 (2011/04/25)
An efficient, safe and scalable procedure for the continuous flow thermolysis of azidoacrylates to yield indoles has been developed and was applied to the synthesis of related heterocycles. The scalability of the process was demonstrated in the continuous flow synthesis of a precursor to the DAAO inhibitor 4H-furo[3,2-b]pyrrole-5-carboxylic acid.
Structural necessity of indole C5-O-substitution of seco-duocarmycin analogs for their cytotoxic activity
Choi, Taeyoung,Ma, Eunsook
, p. 7971 - 7984 (2011/03/22)
A series of racemic indole C5-O-substituted seco-cyclopropylindole (seco-CI) compounds 1-5 were prepared by coupling in the presence of EDCI of 1-(tertbutyloxycarbonyl)- 3-(chloromethyl)indoline (seg-A) with 5-hydroxy-, 5-O-methylsulfonyl, 5-O-aminosulfonyl, 5-O-(N,N-dimethylaminosulfonyl)- and 5-O-benzyl-1H-indole-2- carboxylic acid as seg-B. Compounds 1-5 were tested for cytotoxic activity against four human cancer cell lines (COLO 205, SK-MEL-2, A549, and JEG-3) using a MTT assay. Compounds 2 and 3 with small sized sulfonyl substituents like 5-O-methylsulfonyl and 5- O-aminosulfonyl exhibit a similar level of activity as doxorubicin against all cell lines tested.
β2-Agonists containing metabolically labile groups. II. The influence of ester groups in the aryl system
Albrecht,Heindl,Loge
, p. 57 - 60 (2007/10/02)
β2-Agonists which are derived from alkyl 7-hydroxy-indole-2-carboxylates are highly active bronchodilators. The corresponding carboxylic acids, which can be formed metabolically from the esters, have diminished activity. Thus these compounds ar
