Diastereoselective α—Alkylation of β—Amino Esters：Preparation of Novel α—Substituted β—Amino Esers from α—Amino Acids

Enantiomerically pure α-substituted β-amino esters were prepared from natural L-α-amino acids through Arndt-Eistert homologation and diastereoselective α-alkylation.     

A Facile Synthesis of α-Phenylthio-α,β-Unsatuated Esters

α-phenylthio-α，β-unsaturated esters 6 were synthesized by Witting reaction of 3.which were prepared by a phenylsulfenyllation-trans-ylidation reaction.     

Synthesis of 5—Aryl—1,2—dihydro—1—pyrrolizinones

In order to search for new potent anti-inflammatory and analgesic agents in pyrrolizinones,the title compounds were designed and synthesized.A series of the compounds were prepared with two different synthetic schemes.Some of the compounds showed remarkable anti-inflammatory and/or analgesic activities on mice.     

Synthesis of 4—Aryl—3,4—dihydropyrimidinones Using Microwaveassisted Solventless Biginelli Reaction

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O，O—二（β，β′—二叠氮异丙基）—α—对甲苯磺酰氨基—间硝基苄基磷酸酯的合成及晶体结构

首次合成了标题化合物C20H23N14O7PS，并通过元素分析、IR和^1H NMR对化合物进行了表征，用X射线单晶衍射法测定了该化合物的晶体结构。晶体中一个不对称单元内有四个结晶学上独立的分子，这四个分子的构型基本相同。每两个分子之间以一对N－－H…O氢键连接，生成一个非中心对称的二聚体，组成二聚体的两个分子侧链局部权象存在明显的差异。整个晶体则是由这些二聚体以van der Waals作用力堆积而成。     

1，5—苯并硫氮杂卓—α—氨基—β—内酰胺衍生物的合成及立体结构（Ⅱ）

用一种甘氨酸N－端保护试剂和1，5－苯并硫氮杂卓反应，合成了51，5－苯并硫氮杂卓－α－氨基－β－内酰胺衍生物，其结构经元素分析、^1H NMR，MS和IR确证，用X射线衍射法确定了产物的立体结构，结果表明，该反应具有立体专一性，四元环上的两个取代基位于环的同侧，为顺式结构，产物分子中的七元环为稳定的类椅式构象。     

A Facile Synthesis of 3,5—Diaryl 1,2,4—Selenadiazoles from Aryl Selenoamides

A facile synthesis of 3,5-diaryl 1,2,4-selenadiazoles was provided by treatment of aryl selenoamides with p-methylphenyl sulfonyl chloride in chloroform.     

微波快速合成α—巯基—β—（4—甲氧基）苯基丙烯酸

１引言α－巯基－β－（４－甲氧基）苯基丙烯酸是一种高灵敏度、高选择性的显色剂，可用于痕量镍的测定［１］，也是一种重要的有机合成中间体。本文报道在微波辐射条件下由对甲氧基苯甲醛和绕丹宁快速缩合成对甲氧基苯亚甲基绕丹宁，然后对甲氧基苯亚甲基绕丹宁在氢氧化...     

Stereocontrolled Synthesis of (E)-β,γ-Unsaturated Esters via Palladium-Catalyzed Cross-Coupling of (E)-Alkenylboronic Acids with α-Bromoacetic Esters

The cross-coupling reaction of trans-alkenylboronic acids with a-bromoacetic esters was firstly studied. It was found that using Pd(OAc)2 as catalyst, a bulky electron-rich phospine, (2-dicyclohexylphospino-biphenyl) as ligand, the reaction can be readily accomplished to give specific (E)-b,g-unsaturated esters in high yields.     

5-雄烯-3β, 7α, 17β-三醇和5-雄烯-3β, 7β, 17β-三醇的合成

以5-雄烯二醇为原料,用微生物转化的方法合成了两个重要的神经甾体5-雄烯-3β, 7α, 17β-三醇和5-雄烯-3β, 7β, 17β-三醇。所用菌种总枝毛霉为我们自己筛选,并首次应用于5-雄烯-3β, 7α, 17β-三醇和5-雄烯-3β, 7β, 17β-三醇的合成中。     

Selective α-Bromination of β-Keto Esters in Reusable PEG-400 under Mild and Catalyst-free Conditions

An efficient bromination protocol for the synthesis of α-bromo-β-keto esters has been developed. In PEG-400 （poly（ethylene glycol-400））, a variety of β-keto esters were treated with NBS （N-bromosuccinimide） at room temperature to selectively afford the corresponding α-monobromination products in excellent yields. It is noteworthy that the reaction was conducted under mild, environmentally benign and catalyst-free conditions.     

Facile Preparation of Homoallyl β′，γ′—Unsaturated Amines via 1,2—Addition of α，β—Unsaturated Imines with Allylsamarium Bromide

A series of homoallyl β′，γ′-unsaturated amines were synthe sized via 1,2-addition of α，β-unsaturated imines with allylsamarium bromide in excellent yields under mild and neutral conditions.     

KF-蒙脱土催化下丙二腈与α,β-不饱和酮的迈克尔加成反应

本论文研究了KF-蒙脱土催化下丙二腈与α,β-不饱和酮的迈克尔加成反应,研究发现在不同的反应温度下可以得到加成和环化两种不同的产物。该方法和现有的方法相比具有产率高、反应条件温和、操作简单、试剂易得等优点。     

SmI2－Mediated Addition Reaction of α－Halomethylsulfones to Carbonyl Compounds. A Convenient Synthesis of β－Hydroxysulfones

Due to the chemoselective dehalogenation by SmI2, the addition of a-halomethylsulfones to carbonyl compounds afforded ,β-hydroxysulfones. Those reactions with α-bromomethylsulfones gave the products in moderate to good yields. The SmI2-mediated addition of gem-dihalomethylsulfones to ketones also afforded α-halo-β-hydroxysulfones in moderate yields.     

胆甾-4α-甲基-8-烯-3β，7α-二醇二乙酸酯的结构与性质研究

Lophenol, cholest-4α-methyl-7-en-3β-ol (1), obtained from Dracaena cochinchinensis (Lour.) S. C. Chen, was structurally modified. It was acetylated to protect 3β-hydroxyl group, and then oxidised by selenium dioxide in acetic acid to give cholest-4a-methyl-8-en-3β, Ta-diol diacetate (3). This compound 3 is unstable in chloroform solution or when heated and easily converted to a diene compound, cholest-4a-methyl-7,14-dien-3β-ol acetate (4). The structures of 3 and 4 were elucidated by means of IR, ^1H NMR, ^13C NMR and MS, and the absolute configuration of 3 was established by X-ray crystallography. The property of 3 was also discussed in this paper. Both 3 and 4 are new compounds and were reported for the first time.     

Highly Enantioselective Iridium‐Catalyzed Hydrogenation of α,β‐Unsaturated Esters

α,β‐Unsaturated esters have been employed as substrates in iridium‐catalyzed asymmetric hydrogenation. Full conversions and good to excellent enantioselectivities (up to 99 % ee) were obtained for a broad range of substrates with both aromatic‐ and aliphatic substituents on the prochiral carbon. The hydrogenated products are highly useful as building blocks in the synthesis of a variety of natural products and pharmaceuticals.     

聚合物负载磺酸催化的三组分反应合成1-酰胺烷基-2-萘酚

聚合物负载磺酸，一种环境友好的固体酸催化剂，可以有效地催化2-萘酚、脲或酰胺和醛的三组分“一锅”反应生成1-酰胺烷基-2-萘酚。该方法得率高，操作简单。     

无金属和未催化的Hantzsch酯还原 a, b-不饱和酮反应

Hantzsch酯和 a, b-不饱和酮在氩气保护下,直接在二甲苯中回流可以得到相应的饱和酮,整个过程不需要加入任何金属或有机催化剂。