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氨基苯乙酮

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Goal compound synthesis namely: Take the vanillic acid as outset raw material, obtains 4- hydroxyl - 3- anisole methyl formate with the methyl alcohol reflux conditions, then after the etherification, the nitration, the return to original state, the ring closure response obtains 6- methoxy - 7- animal pen oxygen radical kui zuo lin - 4- alkone, then passes through the chlorination, the substitution aniline, to escape responses again and so on animal pen oxygen radical, etherification to obtain the goal compound; The goal compound and the diethylamine had the amine substitution reaction to obtain TM1, namely 4- benzene amino - 6- methoxy - 7- [2- hydroxyl - 3-(N, N- two ethyl aminos) third oxygen radical] kui zuo lin; Through zuo has the etherification with the Austria niter to respond obtains TM2, namely 4- benzene amino - 6- methoxy - 7- [2- hydroxyl - 3-(2- methyl - 5- nitryl imidazole) third oxygen radical] kui zuo lin.

目标化合物的合成即:以香草酸为起始原料,与甲醇回流条件下得到4-羟基-3-甲氧基苯甲酸甲酯,然后经过醚化、硝化、还原、环合反应得到6-甲氧基-7-苄氧基喹唑啉-4-酮,然后再经氯化、取代苯胺、脱苄氧基、醚化等反应得到目标化合物;目标化合物与二乙胺发生胺取代反应得到了TM1,即4-苯氨基-6-甲氧基-7-[2-羟基-3-丙氧基]喹唑啉;通过与奥硝唑发生醚化反应得到TM2,即4-苯氨基-6-甲氧基-7-[2-羟基-3-(2-甲基-5-硝基咪唑)丙氧基]喹唑啉。

Based on the synthesis method and the function of decreasing blood glucose levels of rosiglitazone, and the report on benzoquinones which resulted in a significant decrease in blood glucose levels, a novel non-thiazolidinedione class of PPARy agonist 2, 5-Dihydroxy-3-{4-[2-(methyl- pyridin-2- yl-amino)- ethoxy] -phenyl}-6-phenyl-[l, 4] benzoquinone (4) was designed and synthesized.

在合成罗格列酮的基础上,根据某些醌类结构化合物的类似胰岛素作用,设计并合成了一种非噻唑烷二酮类PPARγ激动剂2,5-二羟基3-{4-[2-(甲基-2-吡啶氨基)-乙氧基]-苯基}-6-苯基-1,4苯醌(4)。

Bezaldehyde was used as protective agent in first method.S-Epichloeohydrin was aminated and acidulated to give(2S)-1-Amino-3-chloro-propanol Salts.The acetylation of (2S)-1-Amino-3-chloro-propanol by acetic anhydride produced the intermediate-N-[2--3-chloropropyl]acetamide.And then at 20℃,in the presence of lithium tert-butoxide,benzyl 3-fluoro-4-morpholinophenyl carbamate react with-N-[2--3-chloropropyl]acetamide to give linezolid in total yield of 43.6%.

路线一采用苯甲醛作保护剂,使S-环氧氯丙烷氨解、酸化生成S-1-氨基-3-氯-2-丙醇盐酸盐,然后经乙酰化反应后,生成中间体-N-[2-乙酰氧基-3-氯丙基]乙酰胺,再用N-(3-氟-4-吗啉苯基)氨基甲酸苄酯和中间体在催化剂叔丁醇锂存在下25℃反应生成利奈唑酮,总产率达到43.6%。

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