2-[二-(2-氯乙基)-胺基]-5-苄氧基-1,3,2-氧氮磷杂环己烷-2-氧化物的不对称合成

2-[二-(2-氯乙基)-胺基]-5-苄氧基-1,3,2-氧氮磷杂环己烷-2-氧化物是抗癌药物Endoxan的衍生物,其光学异构体的合成已有报道.本文报道了我们从廉价易得的手性原料天然-L-酒石酸开始,通过较为简捷的合成路线,完成了对目标化合物全部4个光学异构体的合成.化合物的有关数据参见表1.     

Pd(O) promoted transformation of N-tosyl-2-(1,3-butadienyl)-aziridine into N-tosyl-2-vinyl-3-pyrroline

1,3-Butadienylaziridines activated by N-tosyl group smoothly rearrange to vinylpyrrolidine derivatives in the presence of a catalytic amount of Pd(PPh₃)₄. Transformation of dienylazetidines into vinylpiperidine derivatives is also described.     

A theoretical study on 1-(thiophen-2-yl-methyl)-2-(thiophen-2-yl)-1H-benzimidazole

The molecular geometry and vibrational frequencies of 1-(thiophen-2-yl-methyl)-2-(thiophen-2-yl)-1H-benzimidazole (C(16)H(12)N(2)S(2)) in the ground state has been calculated using the Hartree-Fock (HF) and density functional method (B3LYP) with 6-31G(d) basis set. The optimized geometric bond lengths and bond angles obtained by using HF and DFT (B3LYP) show the best agreement with the experimental data. Comparison of the observed fundamental vibrational frequencies of 1-(thiophen-2-yl-methyl)-2-(thiophen-2-yl)-1H-benzimidazole (C(16)H(12)N(2)S(2)) and calculated results by density functional B3LYP and Hartree-Fock methods indicate that B3LYP is superior to the scaled Hartree-Fock approach for molecular vibrational problems.     

Synthesis and properties of 1-(2-bromoethyl)-, 1-(2-alkoxyethyl)- and 1-(2-dialkylaminoethyl)2-alkylpyrroles

The reaction of 3-chloropropenyl alkyl ketones or 2,3-dichloropropyl alkyl ketones with 2-substituted ethylamine derivatives leads to the formation of the hitherto unknown 1-(2-R-ethyl)-2-alkylpyrroles.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1047–1049, August, 1990.     

Stereoselective synthesis of 4-(N-mesylamino)-2,3-unsaturated- alpha-O-glycosides via a new glycal-derived vinyl alpha-N-(mesyl)-aziridine

[reaction: see text] N-Mesyl aziridine 7alpha, a new activated vinyl aziridine derived from d-glucal, has been synthesized by cyclization of trans-N,O-dimesylate 6 with t-BuOK in anhydrous benzene. The reaction of 7alpha with alcohols, phenol, and monosaccharides (O-nucleophiles) leads to the corresponding 4-N-(mesylamino)-2,3-unsaturated-O-glycosides and disaccharides through a completely regioselective 1,4-addition process that proceeds with high or complete alpha-stereoselectivity.     

Synthesis of 6-Methyl-4-(1-methyl-2-buten-1-yl)-2-(2-cyclohexen-1-yl)- and 6-Methyl-4-(1-methyl-2-buten-1-yl)-2-(1-cyclohexen-1-yl)anilines

Alkenylation of 6-methyl-2-(2-cyclohexen-1-yl)- and 2-(1-cyclohexen-1-yl)anilines with piperylene in the presence of AlCl₃ and transformation of the resulting cyclohexenylanilines into carbazole structures were studied.__________Translated from Zhurnal Prikladnoi Khimii, Vol. 78, No. 3, 2005, pp. 441–443.Original Russian Text Copyright © 2005 by Gataullin, Ishberdina, Sotnikov, Abdrakhmanov.     

1-(2′-triethylsilylethyl)-, 1-(2′-triethylsilylvinyl)-, and 1′-(2′-triethylsilylethynyl)-silatranes

Conclusions The reaction of 2-triethylsilyl-substituted ethyl-, vinyl-, and ethynyltrialkoxysilanes with triethanolamine gave 1-substituted silatranes possessing neurotropic activity.Translated from Izvestiya Akademii Nauk SSSR, Seriya Khimicheskaya, No. 11, pp. 2611–2613, November, 1984.