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Unusual heterocyclization of chalcone podands with 3-amino-1,2,4-triazole

“…Retention times for compounds were as follows: 16.9 min (for 8), 20.7 min (for 6), 2)). 13 C NMR, δ: 39.65 (C(24)); 41.59 (C(20)); 41.90 (C(20a)); 54.67 (C(4a)); 65.31, 66.75, 68.50, 68.86 (C(14), C(13), C(11), C(10)); 110.29 (C(16)); 111.84 (C(8)); 119.53 (C(18)); 120.37 (C(6)); 123.74 (C(4b)); 124.81 (C(5)); 127.06 (C(19a)); 127.25 (C(2´)); 127.49 (C(3´)); 127.77 (C(2´´)); 128.27 (C(17)); 128.68 (C(3´´)); 129.57 (C(7)); 131.06 (C(19)); 131.27 (C(4´)); 133.12 (C(4´´)); 136.54 (C(1´´)); 136.98 (C(1´)); 151.79 (C(2)); 154.29 (C(22a)); 154.84 (C(8a)); 156.08 (C(15a)); 177.39 (C(21)); 199.55 (C (23) X ray diffraction study. Crystals of triazolopyrimidine po dands 4-6 were obtained by the slow concentration of their solutions in DMF-butanol (1 : 1), whereas crystals of 6,7 di hydro 1,2,4 triazolo[1,5 a]pyrimidine crownophane 7 -of its solution in acetonitrile.…”

Three‐Component Uncatalyzed Eco‐Friendly Reactions for One‐Pot Synthesis of 4,7‐Dihydro[1,2,4]triazolo[1,5‐a]pyrimidine Derivatives

“…The general method for the synthesis of [1,2,4]triazolo[1,5‐ a ]pyrimidine involves cyclocondensation of aminotriazole with α,β‐unsaturated carbonyl compounds . As a part of our interest in using the simple methods for the synthesis of various heterocyclic compounds , a very simple, green, and efficient method for the development of a one‐pot synthesis of [1,2,4]triazolo[1,5‐ a ]pyrimidine derivatives by three‐component condensation of aliphatic, various aromatic, and heterocyclic aldehydes with 1,3‐dicarbonyl compounds (ethyl acetoacetate, acetyl acetone, and diethyl malonate) and 5‐amino[1,2,4]triazole have been reported.…”

A Substituted Tetrahydro-Tetrazolo-Pyrimidine Is a Specific and Novel Inhibitor of Hepatitis B Virus Surface Antigen Secretion

“…Because it is likely that only one of the stereoisomers is biologically active, it is possible that the EC 50 of this compound may actually be four times lower than our determinations for either HBF-0259 or any of the analogues that we have tested, if it is assumed that approximately equal portions of each isomer are present. However, the original synthesis of the HBF-0259 family was described as favoring the formation of the cis isomers (12), and therefore, it is likely that our sample consists mostly of molecules in the two possible cis conformations. To address these points, we are moving in two separate directions, in conjunction with commercial vendors: (i) we will attempt separation of the mixture by chiral chromatography, with subsequent testing of the isolated stereoisomers in our primary ELISA, and (ii) analogues of IHVR compounds modified by insertion of double bonds into the tetrahydropyrimidine ring to reduce or eliminate the chirality will be synthesized and tested.…”