4-咪唑甲酸乙酯的制备

甘氨酸经乙酰化、酯化，在氢化钠作用下与甲酸乙酯缩合，然后在盐酸条件下与硫氰酸钾关环，最后通过双氧水氧化脱巯基，得到咪唑甲酸乙酯，总产率为13％．产物经核磁、元素分析表征．     

两种双脯氨醇的合成

以1,3 二溴丙酮与脯胺醇为原料合成了两种新型手性氨基醇1,3 双[(2S) (二苯基羟甲基) 1 四氢吡咯基]丙酮1和1,3 双[(2S) (二苯基羟甲基) 1 四氢吡咯基] 2 丙醇2,总产率分别为39%和35%.     

两种新型手性氨基醇的合成

L-脯氨酸经3步反应制得手性氨基醇(S)-(二苯基羟甲基)四氢吡咯。该化合物分别与苄溴及β-溴甲基萘反应得到两种手性氨基醇二苯基-[(S)-1-苄基四氢吡咯基]甲醇和二苯基-[(S)-1-(β-萘甲基)四氢吡咯基]甲醇，产率分别为41．1％和32.5％。     

两种N-保护赖氨酸的合成

L-赖氨酸盐酸盐与硫酸铜反应形成赖氨酸铜盐,继而与醋酐反应,得到Nε-乙酰基-赖氨酸铜盐,再利用H2S将铜脱去,最后用(Boc)2O或Fmoc-OSu保护α-氨基,得到Nε-乙酰基-Nε-叔丁氧羰基赖氨酸Boc-Lys(Ac)-OH(1)和Nε-乙酰基-Nε-芴甲氧羰基赖氨酸Fmoc-Lys(Ac)-OH(2).     

三种L-丙氨酰Betti碱的合成

从L-丙氨酸出发,合成了3个手性Betti碱的L-丙氨酰衍生物.该反应条件温和,操作简单,目标产物产率较高.     

MICROWAVE IRRADIATED ALKYLATION OF DIETHYL ACETAMIDOMALONATE

Ethyl acetamidomalonate was alkylated using three alkylating agents, both by microwave irradiation of a mixture of the malonate , the alkylating agent, potassium carbonate, TEBA, and DMF for 0. 5 to 1. 5 min and by heating a solution of the malonate , sodium ethoxide, and the alkylating agent in ethanol for several hours. The two methods gave, comparable results.     

甲磺酸雷莎吉兰的合成

1-茚酮经不对称诱导、催化加氢合成(R)-1-氨基茚,然后与3-溴丙炔、甲烷磺酸反应制得抗帕金森病新药甲磺酸雷莎吉兰,总产率32%.     

二氢吡啶衍生物的合成

一组取代１，４－二氢吡啶由乙酰乙酸酯类，３－氨基－丁烯酸酯及苯甲醛运用不饱和胺缩合法合成。     

新型双官能团有机小分子催化剂的设计合成

基于天然L-氨基酸的基本结构，设计了一系列双官能团的有机小分子催化剂，并以天然氨基酸为起始原料，经过多步反应合成了这些目标化合物，产物结构经核磁分析正确．     

SUBSTITUENT EFFECTS IN THE BIRCH REDUCTION REACTION OF SUBSTITUTED BENZENES

The substituent effects in the Birch reduction reaction of substituted benzenes are discussed. A nonplanar^boat-form conformation is suggested for the benzene radical union formed by the transfer of an electron to a substituted benzene-molecule. In this conformation the 1,4 -dienyl radical union has two double bonds isolated,the negative charge is localized on po-sion 6 and the. single electron is on position 3.the farthest position from the negative charge, when the substituent is electron-withdrawing. Both alkyl and alkoxy groups are considered to be electron-withdrawing. These sub-stituents should be activating groups for their inductive effect. The reaction rate decreasing of alkyl benzenes may be caused by reasons other than electronic effect. The reduction of benzole acid and. benzamide, in which 1,4-dihydro benzenes are obtained,is considered to be an exceptional example,in which an extra stabilized Y-aromatic radical union may be involved.