A direct ortho‐Csp2‐H acylmethylation of 2‐aryl‐2,3‐dihydrophthalazine‐1,4‐diones with α‐carbonyl sulfoxonium ylides is achieved through a RuII‐catalyzed C−H bond activation process. The protocol featured high functional group tolerance on the two substrates, including aryl‐, heteroaryl‐, and alkyl‐substituted α‐carbonyl sulfoxonium ylides. Thereafter, 2‐(ortho‐acylmethylaryl)‐2,3‐dihydrophthalazine‐1,4‐diones were used as potential starting materials for the expeditious synthesis of 6‐arylphthalazino[2,3‐a]cinnoline‐8,13‐diones and 5‐acyl‐5,6‐dihydrophthalazino[2,3‐a]cinnoline‐8,13‐diones under Lawesson's reagent and BF3⋅OEt2 mediated conditions, respectively. Of these, the BF3⋅OEt2‐mediated cyclization proceeded in DMSO as a solvent and a methylene source via dual C−C and C−N bond formations.

In a one-pot self-assembly reaction of Co(OAc)2·4H2O, thiophene-2,5-dicarboxylic acid (H2tdc) and four different bis(tridentate) polypyridyl spanning ligands under ambient conditions, a series of structurally diverse metal-organic frameworks has been synthesised...

There is a paradigm shift in the preformulation drug development strategy of the pharmaceutical industry to engineer the desired dosage form by solid-state manipulation. Cocrystallization is one approach that has been applied in the present study to fortify the poor biopharmaceutical attributes of one of the leading orally effective anticancer drugs in chemotherapy, Gefitinib (GEF). Two novel pharmaceutical cocrystals were engineered with Generally Regarded as Safe (GRAS) status coformers isonicotinamide (INCT) and vanillin (VAN). These novel cocrystals were characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), fourier transform infrared (FTIR) spectrometry, hot stage microscopy (HSM), field emission scanning electron microscopy (FESEM), and single-crystal X-ray diffraction (SXRD). Crystal structure analysis showed that GEF− VAN had cocrystallized in a 2:1 ratio, whereas in the case of the cocrystal hydrate of Gefitinib with isonicotinamide (GEF−INCT) the asymmetric unit showed a stoichiometric ratio of drug/coformer/water of 1:1:2. Both cocrystals showed improvement in intrinsic dissolution, maximal serum concentration, and cell inhibition response as compared to a drug, with GEF−INCT•2H 2 O showing better results than GEF−VAN. Such an improvement of biopharmaceutical properties with good stability via these new solid forms of GEF produced by cocrystallization strengthens the claim of novel drug formulation.

Supramolecular isomerization in coordination polymers is demonstrated by using bis(tridentate) polypyridyl ligands and bent dicarboxylate linkers.

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