缩二氨酸

Result s:10 μmol/L retinoids could inhibit the Bel-7402 proliferation and decrease the colony forming of liver cancer cells on soft agar significantly.So some biochemical markers indicating the proliferation status of liver cancer cells changed significant ly, including the significant activity increase of ornithine carbamyl transferase, tyrosine-α-ketoglutaric transaminase and alkaline phosphatase, the significant decrease α-fetoprotein secretion,γ-glutamyltranspetidase and aldolase activity.

结果：10μmol/L维甲酸显著抑制肝癌细胞增殖，并使肝癌细胞软琼脂集落形成率明显减少，使代表肝细胞分化的酶鸟氨酸氨基甲酰转移酶、酪氨酸-α-酮戊二酸转氨酶和碱性磷酸酶比活力明显升高，甲胎蛋白分泌量、γ-谷氨酰转肽酶和醛缩酶比活力明显下降。

This technique pro-duced not only N-phosphonomethyliminodiacetic acid with high quality but also a great deal of chloromethane by the hydrolyzation of dimethyl phosphite and methylal .

提供了一种利用亚磷酸二甲酯残液(亚磷酸二甲酯生产过程中的副产)和甲缩醛(甘氨酸法生产草甘膦过程中的副产)为原料来合成双甘膦的方法，采用该工艺可以合成高含量的双甘膦，而且利用亚磷酸二甲酯残液和甲缩醛的充分水解可生成大量的氯甲烷，从而大大提高上述副产物的综合利用价值，具有很好的发展前景。

hydantoin was synthesized from diethyl malonate comprising condensation with 1, 2-dichloroethane, ammonolysis to diamide, Hoffmann degradation to give 5-cyclopropanespirohydantoin, and ring-opening with 40% hydrobromic acid.

以丙二酸二乙酯为原料，先与1， 2-二氯乙烷缩合生成1， 1-环丙烷二羧酸二乙酯，再经氨解生成1， 1-环丙烷二甲酰胺，然后在次氯酸钙溶液中进行Hoffmann降解成环生成5-环丙螺海因，最后在40%氢溴酸中开环得到5-溴乙基海因。

Furthermore, the important fragment which is composed of pentenyl cinnamic acid and D-Tyrosine, and the ester which is composed of L-N-methylated phenyl amino acid and diketopiprazine was synthesized with considerable yield The conjugation of the new DOPA analogue into the peptide in the total synthesis of Pepticinnamin E was investigatited

另外，本文作者还进一步合成了高收率的戊烯基肉桂酸衍生物与D-酪氨酸的缩合片段及L-N-甲基苯丙氨酸与哌嗪二酮的酯两个重要的结构组成部分；对新多巴衍生物片段嵌入肽链中的工作亦进行了有益的尝试。

After esterification, the ethyl-2-chloro-3-phenylpropionate reacts with diethyl malonate under the catalysis of sodium ethylate, and we obtain the corresponding triethyl ester. The-benzylsuccinic acid is formed by the triethyl ester reacting with concentrate hydrochloric acid and taking place hydrolyzation and decarboxylation reaction at the same time. In order to avoid the formation of cinnamic acid, the sodium ethylate and diethyl malonate must be react sufficiently. The course has simple operation, inexpensive materials and better yield.

具体制备工艺为：首先以L-苯丙氨酸为原料采用重氮化方法得到-2-氯-3-苯基丙酸，再经酯化得到-2-氯-3-苯基丙酸乙酯后在乙醇钠催化作用下和丙二酸二乙酯缩合，发生SN2反应，得到相应的三乙酯，然后经水解和脱羧，得到-苄基丁二酸；在实验中乙醇钠要和丙二酸二乙酯充分反应，避免生成肉桂酸乙酯；该过程操作简单，原料便宜，产率较高，总收率可达到26.8%。

ABSTRACT Immobilized penicillin acylase (from E.coli) was used to catalyze 7 phenylacetamido 3 E propenyl cephalosporanic acid hydrolyzation into 7 amino 3 E propenyl cephalosporanic acid. Then, trans APRA was acylated with hydroxyethyl ester of 4 hydroxy D phenylglycine to obtain trans cefprozil.

以7 苯乙酰氨基 3 E 丙烯基 3 头孢菌素 4 羧酸为原料，在青霉素酰化酶作用下，首先酶法水解得到3 E 丙烯基 3 头孢菌素 4 羧酸，过滤固相酶，滤液调pH分离得到反式APRA固体；在青霉素酰化酶作用下，反式APRA再与对羟基苯甘氨酸乙二醇酯缩合，得到反式头孢丙烯；酶法合成所得的产品与进口反式头孢丙烯对照品一致。

We make chloroacetylaion to N-terminal of Asp, and then convert this compound to GD dipeptide by aminolysis. Followed the lipase -catalyzed peptide synthesis of RGD in aqueous water-miscible organic cosolvent is studied. We set up a new efficient reaction method to synthesize RGD tripeptide. The problem that peptide containing polar amino acid can not be synthesized readily in organic solvent was solved. We offer a new experimental proof for PPL-catalyzed peptide synthesis and make a more general analysis for the effect of some factors in theory.

采用氯乙酰基保护天冬氨酸，然后进行氨解生成GD二肽，利用猪胰脂肪酶催化合成RGD三肽，着重解决了亲水氨基酸/肽片段底物的溶解性与合成产率低的问题，建立了一种新的有效合成RGD三肽的反应模型，并探索解决了极性较强的氨基酸的酶促肽合成的问题，对脂肪酶催化合成肽的影响因素从理论上作了较全面的分析，为肽片段的缩合反应提供了一种新思路。

Four phenylalanine derivatives were synthesized with this approach. The condition of the condensation reaction was optimized. The side reaction of the Curtius reaction was studied and a urine by-product was isolated and characterized.b. Through the detailed study of the behavior of various N-acetyl phenylalanine methyl esters under the condition of the Bischler-Napieralski reaction, it was found for the first time that the formation of benzyl oxazole derivatives was a competitive approach with the normal B-N reaction.

一、基于Bischler-Napieralski反应设计了以苯丙氨酸衍生物为原料的路线，在这条路线的研究中，主要取得了以下结果：、建立了一条以芳香醛和丙二酸单甲酯为原料，通过缩合、氢化、Curtius等反应制备苯丙氨酸甲酯的通用合成路线，对其中的缩合反应条件及Curtius反应中的副反应进行了深入的研究，利用这条路线合成了四个芳环取代的苯丙氨酸单甲酯衍生物。

The side reaction of the Curtius reaction was studied and a urine by-product was isolated and characterized.b. Through the detailed study of the behavior of various N-acetyl phenylalanine methyl esters under the condition of the Bischler-Napieralski reaction, it was found for the first time that the formation of benzyl oxazole derivatives was a competitive approach with the normal B-N reaction. A convincing mechanism was suggested and a rule governing the reaction was summarized.c.

一、基于Bischler-Napieralski反应设计了以苯丙氨酸衍生物为原料的路线，在这条路线的研究中，主要取得了以下结果：、建立了一条以芳香醛和丙二酸单甲酯为原料，通过缩合、氢化、Curtius等反应制备苯丙氨酸甲酯的通用合成路线，对其中的缩合反应条件及Curtius反应中的副反应进行了深入的研究，利用这条路线合成了四个芳环取代的苯丙氨酸单甲酯衍生物。

In order to obtain versatile ulitity of host molecules, three new chiral calix [4] crown ethers containing aza, thio atoms bearing two chiral sites provided by -cysteine ester were synthesized by the condensation of calix [4] arene diacid dichloride with oligoethylene glycol bridged bis-amino acid methyl ester. All new compounds were characterized by NMR, MS and elemental analysis.

以-半胱氨酸为手性源，利用多甘醇二氯醚在碱性条件下对半胱氨酸巯基进行烷基化反应，成功地合成了多甘醇醚链桥联的半胱氨酸衍生物，醚化反应后，在高度稀释条件下与对叔丁基杯[4]芳烃二乙酰氯进行双功能基缩合反应成功地合成了新型的手性杯[4]含氮、硫杂冠醚，并利用〓H NMR、MS等谱图手段对其结构进行了表征。

Breath, muscle contraction of the buttocks; arch body, as far as possible to hold his head, right leg straight towards the ceiling (peg-leg knee in order to avoid muscle tension).

呼气，收缩臀部肌肉；拱起身体，尽量抬起头来，右腿伸直朝向天花板（膝微屈，以避免肌肉紧张）。

The cost of moving grain food products was unchanged from May, but year over year are up 8%.

粮食产品的运输费用与5月份相比没有变化，但却比去年同期高8％。