N-benzyl tryptanthrin derivative, and preparation method and application thereof

摘要

The present invention relates to an N-benzyl tryptanthrin derivative, and preparation method and use thereof. The N-benzyl tryptanthrin derivative of the present invention is characterized in that the derivative has a structural general formula as represented by formula 1, wherein each group is defined as in the specification. The preparation method of the compound is simple, has mild conditions and high yield, and is suitable for industrial production. The N-benzyl tryptanthrin derivative has good indoleamine-2,3-dioxygenase (IDO) inhibitory activity, and can be used for treating diseases having the pathological feature of IDO-mediated tryptophan metabolism.;

主权项

1. An N-benzyl tryptanthrin derivative, which is characterized in that said derivative has the general structure as shown in Formula 1 below: where R1 corresponds to hydrogen or fluorine; R2 corresponds to —NR3R4; R3 and R4 are each independently selected from the following set: H, substituted or unsubstituted C1-C4 alkyl groups, substituted or unsubstituted C2-C4 alkenyl groups, substituted or unsubstituted C2-C4 alkynyl groups, and substituted or unsubstituted C3-C6 cycloalkyl groups; or R3 and R4 together with an adjacent nitrogen atom form a substituted or unsubstituted 5-7 membered heterocyclic ring, where said 5-6 membered saturated ring includes 1-2 nitrogen atoms as well as 0-2 heteroatoms selected from the following set: O and S; substitution refers to cases in which one or more hydrogen atoms present on a given group are substituted by a substituent selected from the following set: C1-C4 alkyl groups, C1-C4 haloalkyl groups, amino-protecting groups and halogens.