2-[1-(叔丁氧羰基氨基)乙基]噻唑-4-甲酸甲酯的合成

以(S)-丝氨酸和N-Boc-(S)-丙氨酸为原料,经酯化、偶合、TBS保护、硫化、脱保护、环合,脱氢等七步反应,合成了对人体肿瘤细胞KB和LoVo具有中等细胞毒性的天然环酯肽Obyanamide的噻唑结构片段2-[1-(叔丁氧羰基氨基)乙基]噻唑-4-甲酸甲酯,其ee值大于98%,总收率为21.4%.     

A Convenient Synthesis of Methyl (Z)-1-Carbamoyl-2-ethenylcyclopropanecarboxylate and (Z)-1-Carbamoyl-2-ethenylcyclopropanecarboxylic Acid

A simple method for the preparation of the title compounds via the reaction of dimethyl 2-ethenylcyclopropane-1,1-dicarboxylate with 6M ammonia in methanol is described.     

Reactions of Methyl 1-(Bromoacetyl)azulene-3-carboxylate with 2-Hydroxy-benzaldehydes: Synthesis of 1-(Benzofuran-2-yl)-3- methoxycarbonylazulenes

A few compounds containing the 2-arylbenzofuran nucleus, have been isolated from plants.[1] For example,moracins A and B, egonol, homoegonol and (±)-machicendiol are well known.     

1-(2-氰乙基)-2-氧代环戊基甲酸甲酯的选择性水解脱羧

对1-(2-氰乙基)-2-氧代环戊基甲酸甲酯(4)的选择性水解脱羧反应进行了系统研究. 发现上述化合物在碱的催化作用下主要生成开环副产物2-(2-氰乙基)己二酸二甲酯及2-(2-氰乙基)己二酸; 由于氰基在酸性介质中也可发生水解, 因此对1-(2-氰乙基)-2-氧代环戊基甲酸甲酯在酸性情况下水解脱羧的反应条件进行了探索, 发现在4 mol•L－1盐酸介质中, 50 ℃下反应24 h, 以84.0%的收率得到目标产物3-(2-氧代环戊基)-丙腈.     

Synthesis,Crystal Structure and Neuroprotection of Methyl 2-（（4-（2-（2-Methylphenoxy）acetyl）- piperazin-1-yl）-methyl）benzoate①

A new phenoxyacetamide derivative, methyl 2-((4-(2-(2-methylphenoxy)acetyl)piperazin-1-yl)methyl)benzoate(C22H26N2O4, Mr = 382.45), has been synthesized and characterized by 1H NMR, 13 C NMR, H RMS and single-crystal X-ray diffraction. The crystal is of monoclinic system, space group P21/c with a = 11.145(2), b = 13.667(3), c = 13.998(3)A, β = 112.01(3)o, V = 1976.8(7)A3, Z = 4, Dc = 1.285 g/cm3, F(000) = 816, μ = 0.089 mm-1, MoKα radiation(λ = 0.71073 A), the final R = 0.0602 and wR = 0.1533 for 2343 observed reflections with I 2σ(I). Intramolecular C–H···O interactions as well as intermolecular C–H···O hydrogen bonds help to stabilize the crystal structure. The preliminary bioassay results show that the title compound exhibits potent neuroprotective activity.     

Reaction of 3-(3-Arylpropenoyl)-2H-chromen-2-ones with Methyl 1-Bromocyclopentane-1-carboxylate and Zinc

Russian Journal of Organic Chemistry - The reaction of 3-(3-arylpropenoyl)-2H-chromen-2-ones with methyl 1-bromocyclopentane-1-carboxylate and zinc resulted in the isolation, after hydrolysis of...     

Reaction of 2- and 4-(Arylmethylideneamino)phenols with Methyl 1-Bromocyclohexanecarboxylate and Zinc

Russian Journal of Organic Chemistry - 2- and 4-(Arylmethylideneamino)phenols react with Reformatsky reagent, obtained from methyl 1-bromocyclohexanecarboxylate and zinc, to form 3-aryl-2-[2-(or...     

Reformatsky Reaction of 1-Aryl-3-(2-hydroxyphenyl)prop-2-en-1-ones with Methyl 1-Bromocyclohexanecarboxylate

Russian Journal of Organic Chemistry - 1-Aryl-3-(2-hydroxy-5-R-phenyl)prop-2-en-1-ones reacted with the Reformatsky reagent derived from methyl 1-bromocyclohexanecarboxylate to give...