A one step synthesis of functionlized N-acyl anthranilamide via Pd-catalyzed carboxamidation of o-halo substituted N-phenylamide consisting of isocyanide insertion followed by oxidation of the imine intermediate has been achived successfully. Furthermore, at elevated temprature (160 o C) the Pd-catalyzed tandem reaction afforded functionlized quinazolin-4-one in a single step without the isolation of N-acyl anthranilamide and proceed through carboxamidation/de-t-butylation/cyclodehydration cascade. This work extends the application of isocyanide insertion chemistry for synthesizing diverse N-heterocycles by transition metal catalysed sequential reactions in a single step.

A series of novel β‐carboline‐peptide (5 a‐5 f)/ tetrahydro‐β‐carbolines‐peptide (10 a‐10 f) has been synthesized via natural product inspired molecular hybridization approach. All the hybrids were examined for their anti‐leishmanial potential. Most of the screened derivatives exhibited significant in vitro anti‐leishmanial activity against promastigote and intracellular amastigotes (IC50 ranging from 2.43 to 7.61 μM) than the control, miltefosine (IC50 = 8.2 μM), with less cytotoxicity in comparison to the standard drugs (sodium stibogluconate, and miltefosine). Compound 5 a was also able to inhibit Leishmania donovani TR (LdTR). A molecular modeling study based on docking and subsequent binding free energy evaluation was carry out in the active site of LdTR to understand their possible binding site. Our results show that prototype 1(5 a‐5 f) & 2 (10 a‐10 f) represent a new structural lead for anti‐leishmanial Chemotherapy.

Aus p‐Amino‐acetophenon (I) wird durch Thiocyanierung das 4‐Amino‐3‐mercaptoacetophenon (II) hergestellt und mit Acetanhydrid zu (III) kondensiert.

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