Abstract The sulfoximine-based tetrazoles have been synthesized via azido-Ugi four-component reactions of sulfoximines, isocyanides, aldehydes, and TMS-azide in MeOH at 70 °C the presence InCl3. Replacement sulfoximines with sulfonimidamides (SIA) has delivered corresponding SIA-based tetrazole. Interestingly, SIA also acts as a surrogate amine to furnish aminotetrazole by-product.

Starting from 2-imino-N-phenyl-2H-chromene-3-carbox-amide, (1) a series of functionalized chromenes were achieved; such as, 2-ethoxy-2,3-dihydro-3-phenylchromeno[2,3-d]pyrimidin-4-one (2), and 2-hydrazinyl-2,3-dihydro-3-phenylchromeno-[2,3-d]pyrimidin-4-one (3). Furthermore, reactions of (3) with some of laboratory available compounds gave pyrazoles (4 9, 12, 13a, 13b), tetrazoles (11), 2-(2-be...

Rationale. The goal of antihypertensive treatment is to reduce risk of cardiovascular morbidity and mortality. Apart from blood pressure lowering per se, also reducing the activities of the renin-angiotensin system and sympathetic nervous system appears to be important. Angiotensin II receptor blocker drugs (ARBs) have provided a useful class of anti-hypertensive drugs. Eprosartan is a relative...

The reaction of cerium(IV) ammonium nitrate (CAN) with a range of N-(p-anisyl)azoles in acetonitrile or methanol solvents leads to N-dearylation releasing the parent NH-azole and p-benzoquinone in comparable yields. The scope and limitations of the reaction are explored. It was successful with 1-(p-anisyl)pyrazoles, 2-(p-anisyl)-1,2,3-triazoles, 2-(p-anisyl)-2H-tetrazoles, and 1-(p-anisyl)penta...

The AMPAC-GaTech Partnership fosters research aimed at opening and developing new avenues and compounds that fit the American Pacific Corporation (AMPAC)’s potential market. Under this umbrella, we are exploring advanced propellants technologies (ionic liquids, energetic polymers), azide chemistry, and applied polymers (agriculture, biomedical). The novel catalytic preparation of 5-aromatic sub...

The antimycotic clotrimazole, a potent inhibitor of the intermediate-conductance calcium-activated K(+) channel, IKCa1, is in clinical trials for the treatment of sickle cell disease and diarrhea and is effective in ameliorating the symptoms of rheumatoid arthritis. However, inhibition of cytochrome P450 enzymes by clotrimazole limits its therapeutic value. We have used a rational design strate...

An unprecedented formal [3+2] annulation of propargylamides with TMSN3 to deliver functionalized tetrazoles is developed. Oxygen-atom transfer (OAT) from the amide group to the C≡C bond was realized via a NIS-triggered-cyclization/ring-opening cascade pathway. The OAT process enables the amide to serve as a two-atom unit in the reactions. Notably, in situ umpolung of azide occurred when termina...