In an attempt to find a new class of antimicrobial agents, a series of oxygen heterocyclic isocoumarins, dihydroisocoumarins, aromatic / aliphatic amino methyl isocoumarin derivatives having benzoyl group at 3 position in isocoumarin moiety was synthesized using simple appropriate starting material o-acyl benzoic acid and bromoacetophenone derivatives in presence of anhy. K2CO3 in ethyl methyl ...

The addition of o-halobenzoic acids to active internal alkynes proceeds efficiently in the presence of CuCl(2) as a catalyst to give the corresponding isocoumarin derivatives in moderate to good yields. This strategy offers a simple, efficient route to synthesis of the isocoumarin derivatives.

Rhomboid proteases are evolutionary conserved intramembrane serine proteases. Because of their emerging role in many important biological pathways, rhomboids are potential drug targets. Unfortunately, few chemical tools are available for their study. Here, we describe a mass spectrometry-based assay to measure rhomboid substrate cleavage and inhibition. We have identified isocoumarin inhibitors...

Straightforward conversion of (+)-6,8-dimethoxy-3,4-dihydro-3- undecylisocoumarin (3) to the title isocoumarin was carried out. Hydrolytic ring opening of (3) afforded the hydroxy acid (4) which was immediately oxidized to keto acid (5) using chromic acid, Cyclodehydration of (5) afforded the 6,8- dimethoxy-3-undecylisocoumarin (6) which on selective demethylation of 8- methoxy group furni...

The title compound, C(16)H(13)ClO(3), is an important inter-mediate in the conversion of isocoumarin to 3,4-dihydro-isocoumarin. The two aromatic rings are oriented at a dihedral angle of 67.18 (3)°. In the crystal structure, inter-molecular O-H⋯O hydrogen bonds link the mol-ecules into centrosymmetric dimers. There is also a C-H⋯π contact between the benzoic acid and 4-chloro-benzyl rings.

straightforward conversion of (+)-6,8-dimethoxy-3,4-dihydro-3- undecylisocoumarin (3) to the title isocoumarin was carried out. hydrolytic ring opening of (3) afforded the hydroxy acid (4) which was immediately oxidized to keto acid (5) using chromic acid, cyclodehydration of (5) afforded the 6,8- dimethoxy-3-undecylisocoumarin (6) which on selective demethylation of 8- methoxy group furnished ...

Chemotherapy is one of the major approaches for the treatment of cancer. Therefore, the development of new chemotherapy drugs is an important aspect of medicinal chemistry. Chemotherapeutic agents include isocoumarins, which are privileged structures with potential antitumoral activity. Herein, a new 3-substituted isocoumarin was synthesized from 2-iodo-3,5-dimethoxy-benzoic acid and oct-1-yne ...

In this paper we report the synthesis of a new family of 4-alkyl isocoumarin derivatives having bromo carbonyl and amino carbonyl group at 3(rd) position of the heterocyclic ring. Synthesis, spectral analysis and bioactivity of new isocoumarin derivatives are discussed in this paper. Some of the synthesized compounds displayed comparable antibacterial activity and some of the new compounds show...

In the mol-ecule of the title compound, C(16)H(11)FOS, the benzene ring is oriented at a dihedral angle of 89.68 (3)° with respect to the planar [maximum deviation 0.009 (2) Å] isocoumarin ring system. An intra-molecular C-H⋯S inter-action results in the formation of a planar five-membered ring. In the crystal structure, inter-molecular C-H⋯O hydrogen bonds link the mol-ecules into chains paral...

The activation of π-bonds in diynyl esters has been investigated by using soft and hard Lewis acids. In the case of the soft selenium Lewis acid PhSeCl, sequential activation of the alkyne bonds leads initially to an isocoumarin (1 equiv PhSeCl) and then to a tetracyclic conjugated structure with the isocoumarin subunit fused to a benzoselenopyran (3 equiv PhSeCl). Conversely, the reaction with...