Synthesis of 3‐(Pyridin‐4‐Ylmethyl)‐4‐Substituted‐1,2,4‐Triazoline‐5‐Thione

The reaction of the hydrazide of pyridine‐4‐acetic acid with isothiocyanate gave thiosemicarbazide derivatives respectively. Further cyclization with 2% NaOH led to the formation of 4‐substituted 3‐(pyridin‐4‐ylmethyl)‐1,2,4‐triazoline‐5‐thione and 3‐(pyridin‐4‐ylmethyl)‐1,2,4‐triazoline‐5‐thione. The structures of all new products were confirmed by analytical and spectroscopic methods.     

Studies on Thiosemicarbazides and Related Heterocycles(ⅩⅩⅥ)──Synthesis of 3-[5'-amino-1'-(4"-chlorophenyl)-1',2',3'-triazol-4'-yl]-4-aryl-1,2,4-triazoline-5-thiones

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Synthesis,Characterization and Crystal Structure of 4‐Amino‐1,2,4‐Δ2‐triazoline‐5‐thione and its Silver(I) Complex

The reaction of 4‐amino‐1,2,4‐Δ²‐triazoline‐5‐thione (ATT, 1 ) with AgNO₃ in methanol led to the complex [Ag(ATT)₂]NO₃ ( 2 ). 2 was characterized by elemental analyses, ¹H NMR, IR, and Raman spectroscopy as well as single‐crystal X‐ray diffraction. The molecular structure of 1 was also determined by single crystal X‐ray analysis. Crystal data for 1 at ?80 C: space group C2/c with a = 2107.4(2), b = 1425.1(1), c = 688.4(1) pm, β = 104.55(1)°, Z = 16, R₁ = 0.0514, crystal data for 2 at ?80 °C: space group P2₁/c with a = 675.7(1), b = 1321.1(1), c = 1311.2(1) pm, β = 90.03(1)°, Z = 4, R₁ = 0.0437.     

N-(3-苯基2 ,3,4-三唑甲酰氨基)-N'-芳酰基硫脲及其环化产物的合成

以PEG 4 0 0为相转移催化剂 ,通过 2 苯基 1,2 ,3 三唑 4 甲酰基肼与芳酰基异硫氰酸酯的加成反应 ,合成了系列新的酰胺基硫脲衍生物 (3 ) ,3分别在酸性和碱性条件下环化制得相应的 1,3 ,4 噻二唑衍生物和 1,2 ,4 三唑啉 5 硫酮衍生物 ,并经元素分析、IR ,1HNMR和MS确证结构。     

Regioselective and Stereoselective Synthesis of the 3-Aryl-4- phosphoryl-1, 2, 4-triazoline-5-ones

Regioselective cyclization of 1-acylthiosemicarbazides has been shown to be an excellent method for the synthesis of triazoles, thiadiazoles and oxadiazoles, with a variety of potential biological activities1-6 and utilities as pharmacological properties7…     

The first example of a “click” reaction with a carboranyl azide and an olefin

While typical organic azides have long been known to undergo 1–3 dipolar cycloadditions with strained CC multiple bonds, such chemistry has never been reported between organomimetic carboranyl azides and alkenes. Here we show that the carborane o-PhCN₃CB₁₀H₁₀ readily undergoes cycloaddition with norbornene at ambient temperature to afford the corresponding triazole adduct with perfect exo-selectivity. The structure of the ensuing heterocycle was unambiguously determined by multinuclear NMR, correlation NMR, and single crystal X-ray diffraction experiments. This first example of such reactivity demonstrates a method to easily introduce carborane clusters directly to scaffolds of interest, without having an organic spacer between the azide functionality and cluster.     

Facile synthesis of 1,2,4-triazolines via PPh3-triggered reaction of azodicarboxylate with 2-azidoacrylates

A convenient method for the synthesis of 1,2,4-triazolines by triphenylphosphine-triggered reaction of dialkyl azodicarboxylate with 2-azidoacrylates is described. The cascade reaction procedure is general and efficient.