乙基化

Then Doripenem came into the market in the July ,2005. We studied the synthesis of Doripemen.Firstly, we synthesized the chemical 2 from the starting material------o-hydroxylphenylacylamine through Reformastky reaction, alkylation, Diekmann reaction, enolization, esterification and etc. Secondly, we synthesized the chemical 3 from L — hydroxylproline through the protection of carboxyl, amidogen and hydroxyl group, reduction by NaBr, SN_2 substitution and Mitsumobu reaction.

我们以水杨酰胺为起始原料，经Reformatsky反应、烷基化、Diekmann环合、烯醇化、酯化等反应合成双环母核2；再从L-羟基脯氨酸出发，经酯化保护羧基、保护氨基、保护羟基、硼氢化还原酯得醇、Sn2取代和Mitsumobu反应等合成巯基侧链3；最后由化合物3经脱保护、水解得硫醇，和化合物2在二异丙基乙基胺的作用下缩合，最后Pd／C催化脱保护，历经16步反应最终得到产物多尼培南。

Two kinds of water-soluble biomimetic chitosan derivatives with a phosphoramide linkage between glucosamine and choline were prepared through Atherton-Todd reaction under the mild conditions, including zwitterionic phosphorylcholine bound chitosan and acetyl-phosphorylcholine bound chitosan with positive charge. The interaction between chitosan derivatives and calf thymus DNA were inversigated by UV alsorption spectra and circular dichroism spectra.

采用Antherton-Todd反应制备了两种水溶性的磷酰化壳聚糖仿生衍生物：两性的N-磷酸胆碱磷酰化壳聚糖和带正电荷的N-乙基磷酸胆碱磷酰化壳聚糖，并用紫外吸收光谱和圆二色光谱研究了两种胆碱磷酰化壳聚糖衍生物与小牛胸腺DNA的相互作用。

The method involves exposing the cells to a compound having the formula I in which: w is a nucleic acid x is a non-amino acid or non-peptide nucleic acid binding group y is a spacer having a chain length equivalent to 1-30 carbon-carbon single covalent bonds or is absent R4 is H or halogen or CH2O-R3; and R1, R2 and R3 are the same or different and are either hydrogen, methyl, ethyl, alkyl, alkenyl, hydroxylated alkyl, hydroxylated alkenyl groups or ether containing alkyl, alkenyl, hydroxylated alkyl or hydroxylated alkenyl groups optionally being an acyl group having a carbon chain length equivalent to 3-24 carbon atoms saturated or unsaturated, with the proviso that at least one of R1, R2 or R3 includes a group having a carbon chain of 3-24 carbon atoms saturated or unsaturated, or to a compound having the formula II in which: w is a nucleic acid x is a non-amino acid or non-peptide nucleic acid binding group y is a space having a chain length equivalent to 1-30 carbon-carbon single covalent bonds or is absent, R5 is alkyl, alkenyl, hydroxylated alkyl, hydroxylated alkenyl group or ether containing alkyl, alkenyl, hydroxylated alkyl or hydroxylated alkenyl group optionally being an acyl group having a carbon chain length equivalent to 3-24 carbon atoms saturated or unsaturated, with the proviso that R5 includes a group having a carbon chain of 3-24 carbon atoms saturated or unsaturated.

该方法包括使细胞暴露于具有式的化合物，在式中：w是核酸，x是非氨基酸或者非肽核酸结合基团，y是具有等于1―30个碳―碳单共价键的链长的间隔基或者不存在，R4是H或者卤素或者CH2O－R3；R1、R2和R3是相同的或者不同的并且是氢、甲基、乙基、烷基、链烯基、羟基化烷基、羟基化链烯基或者包含烷基、链烯基、羟基化烷基或羟基化链烯基的醚，任选地是来源于具有等于3―24个碳原子的碳链长的饱和或不饱和脂肪酸的酰基，其条件是R1、R2或者R3的至少一个包括具有3―24个碳原子的饱和或不饱和碳链的基团，或者使细胞暴露于具有式的化合物，在式中：w是核酸，x是非氨基酸或者非肽核酸结合基团，y是具有等于1―30个碳―碳单共价键的链长的间隔基或者不存在，R5是烷基、链烯基、羟基化烷基、羟基化链烯基或者包含烷基、链烯基、羟基化烷基或羟基化链烯基的醚，任选地是具有等于3―24个碳原子的饱和或不饱和碳链的链长的酰基，其条件是R5包括具有3―24个碳原子的饱和或不饱和碳链的基团。

Antioxidant 2,2′-methylene-bis(4-ethyl-6-tert-butylphenol) is synthesized by condensation of formalin and 4-ethyl-2-tert-butylphenol which is prepared by alkylation of p-ethylphenol with isobutylene in the presence of phosphoric acid or ion-exchange resin as catalysts.

研究了以对乙基苯酚、叔丁醇为原料，在酸性条件下，进行烷基化反应，合成2 叔丁基 4 乙基苯酚，再进一步缩合成抗氧剂425的工艺条件。

This invention is directed to the-tartaric acid salt of 2-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoroethyl-2,3,3a, 4,6,7-hexahydro-pyrazolo(4,3-c) pyridin-5-yl-ethyl}-2-methyl-propionamide which is a growth hormone secretagogue and as such is useful for increasing the level of endogenous growth hormone.

本发明涉及2－氨基－N－{1－－(2，4－二氟－卞氧甲基)－2－氧代－2－3－氧代－3a－(R－吡啶－2－基甲基－2－(2，2，2－三氟－乙基)－2，3，3a，4，6，7－六氢化－吡唑子基(4，3－c)吡啶－5－基－乙基}－2－甲基－丙酰胺的－－酒石酸盐，它是一种生长激素促分泌素，并且可用于提高内源性生长激素水平。

The pure isomers 3-(1-hydroxyethyl)-8-vinyldeuteroporphyrin Ⅸ and 3-vinyl-8-(1-hydroxyethyl)deuteroporphyrin Ⅸ were obtained from protoporphyrin Ⅸ dimethyl ester.Starting from these two acetylating compounds,eight new porphyrin derivatives were synthesized through an alkyloxy fission reaction.

以原卟啉Ⅸ二甲酯为起始原料，合成并分离得到3-(1-羟乙基)-8-乙烯基次卟啉Ⅸ（Ⅱ1）和3-乙烯基-8-(1-羟乙基)次卟啉Ⅸ（Ⅱ2）二个异构体，两者分别经酰化后与醇进行烷氧裂解反应合成了8个全新的卟啉衍生物。

Methods: 2-ethyl aniline was used as starting material of the synthesis and was processed by acetic anhydride acylation, strong nitric acid nitraction at low temperature, and desacyl synthesis to produce 2-ethyl-5-nitro aniline. The product was then synthesized to 3-methyl-6-nitro-lH-indazole by using ring-closing reaction in the presence of NaNO2, and then ethylated to obtain 2, 3-diethyl-6- nitro-2H-indazole. The latter compound was then reduced by SnC12/Hcl to get target compound 2, 3-diethyl-6-nitro-2H-indazole.

以2-乙基苯胺为原料经醋酐酰化、浓硝酸低温硝化及去酰基保护合成2-乙基－5-硝基苯胺，后用亚硝酸钠关环得3-甲基－6-硝基－1H-吲唑，经硫酸二甲酯甲基化得2，3-二甲基－6-硝基－2H-吲唑，最后用氯化亚锡将其还原得到目标产物，通过1HNMR确定结构与目标产物一致。

The synthesis of alkylcyclohexylbenzoic acid: take the synthesis of ethylcyclohexylbenzoic acid as a typical example. With the AlCl3 as the catalyst, cis+trans acetylcyclohexylbenzene is synthesized from the reaction of acetyl chloride, cyclohexene and benzene.

烷基环己基苯甲酸的合成研究：主要研究了乙基环己基苯甲酸的合成，以乙酰氯、环己烯、苯为原料，三氯化铝为催化剂，合成乙酰基环己基苯，用水合肼、氢氧化钾、一缩二乙二醇经过高温加热还原羰基(Wolff-黄鸣龙还原)，将所得到的乙基环己基苯用乙酰氯进行傅克酰基化得到乙基环己基苯乙酮，所得中间体经过处理之后直接得到反式产物，将反式异构体的乙酰基氧化得到反式烷基环己基苯甲酸。

The optimal operation condition of Friedel-Crafts acylation for product Ⅰ was determined by orthogonal experiment: 0.02mol N-ethyl- carbazol, n Benzoyl chloride/n N-ethyl- carbazol=1.2, n AlCl3/n N-ethyl- carbazol=1.2 , at 25 oC for 3.5h. The yield was 94.6%.

通过正交设计实验，探讨了产物Ⅰ的Friedel-Crafts 酰化的最佳反应条件：N-乙基咔唑为0.02mol时，反应物苯甲酰氯与N-乙基咔唑摩尔配比为1.2。，催化剂AlCl3与N-乙基咔唑摩尔配比为1.2， 25℃下反应3.5h，产率可达94.6%。

Taking the brines from Qinghai Chaerhan salt lakes as raw material, sulfonated kerosine as diluting agent, the experiment of extracting boric acid from brines by 2 - ethyl - 1,3 - haxanediol is carried out. The concentration of extractant,acidity, the ratio of organic phase to brine, the time of extraction and extration isotherm are investigated.

以青海察尔汗盐湖提钾后老卤为原料，以磺化煤油为稀释剂，从萃取剂浓度、酸度、相比、萃取时间、萃取等温线5个方面加以试验，获得了2-乙基-1，3-己二醇从卤水中萃取提硼的最佳试验条件，并与2-乙基己醇和磺化煤油的萃取体系进行比较，得出二元醇的萃取效果高于一元醇的结论。

For a big chunk of credit-card losses; the number of filings (and thus charge-off rates) would be rising again, whether

年美国个人破产法的一个改动使得破产登记急速下降，而后引起了信用卡大规模的亏损。

Eph. 4:23 And that you be renewed in the spirit of your mind

弗四23 而在你们心思的灵里得以更新