A facile synthesis of cyanoguanidines from thioureas

A facile synthesis of cyanoguanidines from corresponding thioureas is reported using 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (water soluble carbodiimide).     

A facile synthesis of sulfinyl chlorides from thiolacetates

Alkyl and aryl thiolacetates are converted smoothly into sulfinyl chlorides by sulfuryl chloride in the presence of acetic anhydride.     

A facile synthesis of piperazines from primary amines

A general procedure is described for converting primary amines to N-substituted piperazines. Reaction of an amine with an N-substituted iminodiacetic acid anhydride (V) yields an iminodiacetic acid monoamide (VI) which closes to a 2,6-piperazinedione (VII) upon treatment with acetic anhydride. The diones are reduced to piperazines with borane-THF. Fourteen examples of this process, using twelve aliphatic or aromatic amines and three iminodiacetic acids, are presented. Yields of piperazines, based upon starting amine, ranged from 21 to 52%. The procedure is rapid and no purification problems were encountered. Alternate methods for preparing the 2,6-piperazinedione intermediates are discussed.     

A facile synthesis of hyperbranched polyimides from 2,6,12-triaminotriptycene

<正>Based on monomer 2,6,12-triaminotriptycene,hyperbranched polyimides with high molecular weight modified with different terminal functional groups were obtained by polymerization of A_2+B_3 system.The prepared hyperbranched polyimides had good solubility in CHCl_3,DMF and THF,and performed no detective T_gs in the range of 50-330℃and high T_ds(5%) above 455℃.     

A facile synthesis of cyclotriveratrylene

Cyclotriveratrylene (CTV) can be readily synthesized by chloromethylation or bromomethylation of dimethoxybenzene with halomethyloctyl ether in the presence of SnCl₄. The reaction provides the trimer exclusively and in high yield. Recrystallizations from benzene or CHCl₃ yielded the solvent inclusion complexes and did not remove other inclusion impurities. Flash chromatography on silica yielded the pure CTV.¹³C NMR shows only five signals and no impurities.     

A facile synthesis of N-sulfinylaldimines

A simple and efficient procedure for the synthesis of N-sulfinylaldimines (sulfinimines) from sulfinamides and aldehydes is described. The reaction was carried out in the presence of t-BuOK or NaOH. The method is applicable for the synthesis of optically active sulfinimines.     

A facile synthesis of muscimol

The psychoactive isoxazole muscimol $\text{10}$ has been synthesized in three steps from propargyl chloride.     

A facile synthesis of cyclononatripyrroles

A facile synthesis of a functionalized cyclononatripyrrole derivative is described. It involves the iodine-catalyzed cyclotrimerization of ethyl 3,3-dimethyl-5,7-dihydro[1,3]dioxepino[5,6-c]pyrrole-6-carboxylate in methanol. The product obtained in this way exists solely in the crown conformation typical of cyclononatripyrroles. However, in contrast to previously reported compounds of this class, it possesses three labile methoxymethyl arms that can be further functionalized under acidic conditions.     

A facile synthesis of cyanophenothiazines

A one-pot synthesis of 1, 3 and 4-cyanophenothiazines and a two-step approach to 2-cyanoisomer have been developed. The condensation of 2-aminobenzenethiol and 2,3 or 3,4-dihalogenobenzonitriles followed by Smiles rearrangement or by intramolecular aromatic substitution gave the desired ring systmes.     

A facile synthesis of ulicyclamide

Ulicyclamide (1), a cytotoxic cyclic peptide from a marine tunicate, has been efficiently synthesized by the solid-phase method using diethyl phosphorocyanidate for the coupling and trimethylsilyl triflate for the final deprotection.     

A facile synthesis of polyfoluoroalkyl-lactonization

2(-Benzoxazolyl substituted cyclopropane derivatives were synthesized in the yield of 73-89% from the reaction of telluronium ylides with chalcones.     

A concise route to phytosphingosine from lyxose

Phytosphingosine was synthesized from the commercially available d-2,3-O-isopropylidene-d-lyxofuranose in 28% overall yield by a six-step procedure. This procedure is expedient and flexible for introduction of other lipid moieties on the phytosphingosine structure to make a variety of derivatives that can support the further exploration of their related biological functions.     

A facile synthesis of 3-trifluoromethyl-1,2,4-oxadiazoles from cyanamides

A safe and facile method for the formation of 3-trifluoromethyl-5-amino-1,2,4-oxadiazoles, via a reversed addition of hydroxylamine to cyanamides, is reported. This two-pot procedure is suitable to scale-up and avoids the hazards associated with trifluoromethyl amidoxime synthesis.     

A facile synthesis of imino-protected cyclic guanidine derivatives from diamines

A convenient one-step synthesis of five-membered or six-membered imino-protected cyclic guanidine via an intramolecular ring-closure reaction of alkyl diamine(2a-2g) with 1,3-diamino-protected methylisothiourea(1a and 1b) was established and investigated.Amino guanidine such as 3-(2-aminoethyl)-1,2-dibenzyloxycarbonylguanidine(4a) has been proved to be the intermediate of the reaction via utilizing mono-protected diamine as starting material.The intramolecular ring closure of 4a results in 2-benzyloxycarbonyliminoimidazolidine(3a).This new one-step synthesis has advantages of simple condition,easy workup procedure and reasonable yield.     

5-四氢呋喃基呋喃的合成

六碳醛糖与1,3-双桐或β-酮酸酯在氯化锌存在下缩合, 再经酸性条件下环化生成50-60%得率的5-四氢呋喃基呋喃类化合物。     

A facile synthesis of polysubstituted pyrroles

alpha-Aminoalkylcuprates prepared from CuX.2LiCl (X = Cl, CN) and 1 equiv of an alpha-lithiocarbamate undergo conjugate addition reactions to alpha,beta-alkynyl ketones in moderate to good yields, affording E:Z mixtures of alpha,beta-enones. Treatment of the conjugate adducts with PhOH/TMSCl in CH(2)Cl(2) effected carbamate deprotection and cyclization to afford a flexible two-step synthesis of substituted pyrroles.     

A facile synthesis of ( -deoxypseudophrynaminol

A one-step synthesis of ( )-deoxypseudophrynaminol, a racemic deoxy analog of the natural product pseudophrynaminol, is described.