保护基

In the first part, we studied the possibility of allyl as the protection group of the hydroxyl in nucleosides.

烯丙基作为糖化学中的一种常用保护基在核酸化学中有一定的应用，曾有人将它作为磷酸酯键及碱基环上羰基的保护基，但作为核苷糖环羟基的保护基还未有研究。

In some cases, its epimer 4 was also obtained. 22 compounds were synthesized, among them 18 were new.3. Using the intramolecular Pictet-Spengler reaction to form the pentacyclic skeleton of Et-743, the byproducts 25 were obtained under various conditions. The structures of them were determined to be 1, 2-dihydro-isoquinoline compounds, and the mechanism of the reaction was proposed.B. The synthesis of the analogs of Et-743Because of the failure of removing the protective groups in compounds 14, the synthetic strategy was adjusted.

对于苄基保护的羟基化合物13a，顺利得到化合物30，然后与不同的羧酸反应得到18个酯化合物33-50；对于苄氧羰基保护的氨基化合物13b，由于脱除保护基的化合物31在空气中不稳定，所以我们采取不经分离纯化，直接与羧酸反应得到酰胺化合物53-62，然后再分别对其C-21位的羰基进行还原氰基化，得到10个酰胺目标化合物63-72，另外，我们还对羟基转化为氨基的反应进行了探索。3。

Methods Starting from 2-chloro-4-nitrophenol and 2- pyridine hydrochlorid, 3-chloro-4-(pyridin-2-ylmethoxy) aniline was obtained via etherization and reduction. The obtained aniline coupled with N-(4-chloro-3-cyano-7-ethoxyquinolin-6-yl) acetamide to give 4-[3-chloro-4-(2-pyridylmethoxy) phenylamino]-3-cyano-7-ethoxy-6-N-acetylaminoquinoline. And then it was deacetylated, followed by reacting with4- but-2-enoyl chloride to yield the target compound neratinib.

以2-氯－4-硝基苯酚和2-氯甲基吡啶为起始原料，经醚化、硝基还原得到3-氯－4-（吡啶－2-甲氧基）苯胺，3-氯－4-（吡啶－2-甲氧基）苯胺与3-氰基－6-乙酰氨基－7-乙氧基－4-氯喹啉反应得到3-氰基－6-乙酰氨基－4-［3-氯－4-（吡啶－2-甲氧基）苯氨基］－7-乙氧基喹啉，3-氰基－6-乙酰氨基－4-［3-氯－4-（吡啶－2-甲氧基）苯氨基］－7-乙氧基喹啉去乙酰保护基后，与-4-二甲氨基－2-丁烯酰氯经酰化反应得到ner-atinib。

Both the protection and deprotective group methods for the amino-group on side chain of a new N-pivot lariat crown ether were studied comparatively.

研究了一种新的氮支套素冠醚侧链上氨基的保护和脱保护基方法，结果表明，由过量乙二胺与对甲苯磺酰氯反应得到的单保护乙二胺（N－对甲苯磺酰基乙二胺4a），经N－烷基化环化反应，然后在氢化铝锂存在下脱除保护基，即可制得最佳产率的N－（2－氨基已基）单氮杂－12－冠－4（1）。

Reaction of 5'-O-p-methoxytrityl-thymidine with 1, 1'-carbonyl-diimidazole gave the 3'-O-carbonylimidazolide, which was condensed in high yield with 3'-O-protected thymidine to give a dithymidine carbonate. In the same way, we obtained the protected trithymidine dicarbonate. After deprotection, we obtained quantatively the trithymidine dicarbonate.By the same stratagy, we completed the synthesis of dithymidine sulfite.It was shown that allyl can be used as a good protection group for hydroxyl of ribose in the synthesis of oligonucleotides consisting in some unstable nucleotide analogues.

我们在第一部分工作的基础上，以烯丙基作为3'-OH的保护基合成了保护的三胸苷碳酸酯以及二胸苷亚硫酸酯，用我们所得的脱保护条件进行了脱保护研究，得到了三胸苷碳酸酯以及二胸苷亚硫酸酯，并研究了它们合成中的一些化学问题，结果表明：烯丙基能很好地运用于这两类寡核苷酸类似物的合成中，其脱保护条件为中性，不会影响碳酸酯键及亚硫酸酯键。

The present invention relates to a novel process for converting the intermediate in the synthesis of atorvastatin having the following formula or atorvastatin lactose into the non-crystalline atorvastatin calcium: wherein A denotes a common protection group or separate protection groups for the dihydroxy group and B denotes a carboxylic acid protection group.

本发明涉及一种将具有下式的阿托伐他汀合成中的中间体或阿托伐他汀乳糖转化为非结晶阿托伐他汀钙的新方法：其中A表示二羟基的共同保护基或单独保护基，而B表示羧酸保护基。

STUDY ON THE APPROACH AND THE MEDCHINE FOR THE DEPROTECTION OF SILYL ETHER BY SODIUM PERIODATE Abstract Silyl ethers are the most widely used hydroxyl protecting groups in organic synthesis.

第二部分：过碘酸钠去硅醚保护基方法及机理的研究硅醚保护基种类多，稳定性较好，且反应简单，作为羟基的保护基在有机合成中得到广泛应用。

L-fucose, as raw material, protected with ortho ester, synthesized the glycosyl acceptor 60, 76, thioglycoside doner 57、61、62, fluorglycoside 65、66 and Schimidt doner 68, 70 in a simple and efficient way.

本文从L-岩藻糖出发，以原酸酯保护的方法简单高效的合成了具有合适保护基的糖基受体60、76，糖基供体57、61、62、65、66、68及70。

By simply stirring L-dopa methyl ester 1 and aldehyde 2 with anhydrous sodium acetate in acetic acid at room temperature for several hours, we obtained the desired 1, 3-syn compound 3 predominantly.

Et-743类似物的合成：由于化合物14 C-1位的保护基没能脱除，所以我们决定调整合成路线，采用了先将化合物13的C-1位的保护基脱除，再将C-21位羰基还原氰基化的策略。

Furthermore, proton singlets of Fmoc group were treated as internal standard because of their station in both starting material and product.

用HR／MAS NMR分析技术不仅跟踪优化了固相羟基氨基酸的糖基化反应条件，而且选择固载在树脂上的糖基化Nα-Fmoc保护羟基氨基酸〓H NMR中最低场，且分辨好的Fmoc保护基信号做为内标，糖上乙酰基的积分面积为标准直接定量了键合在Tenta Gel S NH〓树脂上氨基酸甙化的产率。

In the United States, chronic alcoholism and hepatitis C are the most common ones.

在美国，慢性酒精中毒，肝炎是最常见的。

If you have any questions, you can contact me anytime.

如果有任何问题，你可以随时联系我。