A simple efficient and neat synthesis of α-hydroxy phosphonates has been accomplished from aromatic/ heterocyclic aldehydes and diethyl phosphite using KHSO4 as a catalyst under solvent-free conditions at ambient temperature. These compounds are characterized by spectral and analytical data and tested for their anti-oxidant activity.

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Syntheses of a new series of biologically potent α-aminophosphonates were accomplished by one-pot Kabachnik-Fields reaction using TiO2-SiO2 as solid supported catalyst under microwave irradiation conditions. The chemical structures of all the newly synthesized compounds were confirmed by analytical and spectral (IR, 1H, 13C, 31P NMR, and mass) data. Their anticancer nature was evaluated by screening the in vitro activity on two human cancer cell lines, HeLa and SK-BR-3. Compounds 4i and 4o showed the best activity on these cancer cells even though the majority of the compounds, and particularly 4l and 4p, have good cytotoxic activity against them.

Biologically portent/significant tetrahydrodipyrazolo[3,4‐b:4′,3′‐e]pyridines are synthesized by an efficient green synthesis of various aldehydes with 3‐methyl‐1H‐pyrazol‐5(4H)‐one in ammonium acetate using phospho sulfonic acid as a solid catalyst under microwave‐assisted interaction under solvent‐free conditions at 70°C. This methodology is easy to handle and get good to excellent yields. Later the potential in vitro antiproliferation of the titled compounds is evaluated. Among all the titled compounds, 4s and 4t showed the most potent anticancer potentiality on the used cancer cell lines of SK‐BR‐3 and HeLa (IC50 = 10.70 ± 0.27 and 12.58 ± 0.38, and 19.38 ± 0.32 and 21.55 ± 0.41 μg/mL for SK‐BR‐3 cells lines and HeLa cells lines, respectively), which were comparable to the positive control.

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α-Aminophosphonates(4a-j)were synthesized in one-pot simultaneous reaction of 4-bromo-3-methyl benzenamine (1), dimethylphosphite (3) and different aromatic aldehydes(2a-j)by Kabachnik-Fields reaction in the presence of tetramethylguanidine (TMG) (10 mole%) as catalyst in toluene at reflux temperature afforded4a-jin good yields. All these compounds were found to exhibit moderate to good antimicrobial activity.

A new class of biologically active 13-membered phosphorus-macroheterocycles (6a-l) were conveniently synthesized from 1,2-bis(salicylidene amino)-phenylene (1), by treating with phosporusoxychloride (3) and followed by reacting with various aromatic thiols and amines (5f-l) in one path, and in another path 1 was directly treated with various phosphorodichloridates (2a-e) in the presence of triethylamine at 0-10°C under N(2) atmosphere in THF. All the title compounds were confirmed by analytical and spectral data (IR, (1) H-, (13) C-, (31) P-NMR, and mass spectra) and screened for anti-oxidant activity. Among these compounds, 6k, 6e, and 6l containing nitro, fluoro, and chloro groups as substituents on the phenyl ring exhibited high anti-oxidant activity with effective inhibitory concentration (IC(50) ) values.