【導讀】泛關注并且得到了有關機構的研究應用。本文對吡啶羧酸類配位聚合物進行了研。酸類配位聚合物的制備。熱法、溶劑熱法、流相反應法、溶膠—凝膠法。到了比較全面的認識。

　　

【正文】 oc.,1998,117:9481 9485. [18] Zhao B,Chen X,Cheng P,et Polymers Containing1D Channels as Selective Luminescent Probes ［ J ］ .J. Am. ., 2021, 洛陽理工學院畢業(yè)設計論文 24 126:15394 15395. [19] 張中強 , 黃如丹 , 許顏清等 . 二維網格結構的新型配位聚合物［ Zn（ PDA）］ n 的合成、晶體結構及熒光性質［ J］ . 高等學?；瘜W學報 , 2021, 29（ 8） : 1528 1531. [20] 王艷，吡啶羧酸類配位聚合物的研究進展，化學工程師， 2021,3： 3132. [21] 陳小利 ，新型柔性芳香羧酸類配位聚合物的合成，結構及性質研究： [博士學位論文 ]，西安，西北大學， 2021. [22] Hoskins, B. F., Robson. R. Infinite polymeric frameworks consisting of three dimensionally Linkedrodlike segments [J]. Journal of the American Chemical Society, 1989, 111:59625964. [23] Zhu, X. D., Lu, J., Li, X. J., et al. Syntheses, Structures, NearInfrared, and Visible Luminescence of LanthanideOrganic Frameworks with Flexible Macrocyclic Polyamine Ligands [J].Crystal Growth and Design. 2021, 8: 18971901. [24] Zhang X. M. Hydrothermal in Situ Ligand Syntheses [J]. Coordination Chemistry Reviews, 2021, 249: 12011219. [25] Chen X. M., Tong M. L. Solvothermal in Situ Metal/Ligand Reactions: A New Bridge between Coordination Chemistry and Organic Synthetic Chemistry [J]. Accounts of Chemical Research, 2021, 40: 162170. [26] Yang, J., Ma, J. F., Liu, Y. Y., et al. OrganicAcid Effect on the Structures of a Series Pb(II) Complexes[J]. Inanic chemistry, 2021, 46: 65426555. [27] Daz, P., BeBuchholz, J., Vilar, R., et al. Anion Influence on the Structures of a Series of Copper (II) MetalOrganic Frameworks [J]. Inanic Chemistry, 2021, 45: 16171626. [28] 楊士姚 . 鈷、鎳、銅、鋅離子與芳香羧酸配位聚合物的組裝、結構和性質 [博士學位論文 ]，廈門 :廈門大學 , 2021. [29] 任鵬 . 新型無機及無機一有機雜化二階非線性光學材料的設計、合洛陽理工學院畢業(yè)設計論文 25 成和性能 [博士學位論文 ]. 武漢 :武漢大學 , 2021. [30] 施而畏 , 夏長泰 , 王步國 , 仲維卓 . 水熱法的應用與發(fā)展 . 無機材料學報 ,1996, 11(2), 193. [31] 林君 , 龐茂林 , 韓銀花 , 于敏 , 張洪杰 . 溶膠一凝膠工藝制備法光薄膜究進展 , 無機化學學報 , 2021, 17(2), 153. [32] 王金龍 , 用流變相反應制備芳族羧酸鹽單晶和鎳酸鹽正極材料[碩士學位論文 ]. 武漢 : 武漢大學 , 2021. [33] 袁良杰 . 流變相合成法及其應用研究 [博士學位論文 ]. 武漢 : 武漢大學 , 2021. [34] 李建宇 . 稀土發(fā)光材料及其應用 (第一版 )[M]. 北京 : 化學工業(yè)出版社 . 2021, 2. 洛陽理工學院畢業(yè)設計論文 26 外文資料翻譯 GPR109a agonists. Part 1: 5Alkyl and 5arylpyrazole–tetrazoles as agonists of the human orphan Gprotein coupled receptor GPR109a. Nicotinic acid (niacin) 1 has been a leading treatment for dyslipideamia and for the prevention of atherosclerosis for over 40 Long term clinical studies have revealed niacin’ s ability to reduce mortality from coronary heart In spite of niacin’ s clinical significance, patients treated with niacin show low pliance of use due to an intense flushing side ,4 A number of drug discovery programs have focused on the development of a‘ flushfree’ niacinlike therapy. Despite considerable effort in the field, the absence of a niacinrelated target and/or mechanism of action have limited such investigations. Recently, a Gproteincoupled receptor, GPR109a, was identified as a molecular target for Mechanistic studies have suggested that the benefits of niacin therapy may result from the activation of GPR109a located on Recent experiments have shown that niacin activation of GPR109a results in a reduction of intracellular CAMP and it is believed that this reduction in CAMP levels effectively inhibits iypolysis by the negative modulation of hormone sensitive lipase (HSL). As a result, a conitant decrease in plasma free fatty acid (PFFA) levels is observed and it is thought that this reduction in PFFA is crucial to the lipid modulation and resulting therapeutic value of In control experiments, GPR109a knockout mice, when treated with niacin therapy, failed to show the characteristic reduction in plasma FFA that is observed in wild type mice. Furthermore, these mice also failed to show a niacininduced cutaneous flush. As a result,it has been suggested that the niacinassociated flush and antilipolytic effects are both mediated through In light of these recent findings, we initiated a drug discovery program 洛陽理工學院畢業(yè)設計論文 27 focused on the identification of a ‘ flushfree’ agonist of the niacin receptor. Our lead identification effort identified pyrazole– tetrazole 2 as a promising – 10 While pyrazole 2 displayed only modest in vitro affinity for GPR109a (Table 1), its in vivo pharmacology was intriguing (see Fig. 1).11 In a mouse plasma freefatty acid (pFFA) assay, mice treated with 10 mpk of pyrazole 2 showed a reduction in plasma free fatty acid levels parable to that observed upon treatment with 100 mpk of niacin. Furthermore, in a mouse vasodilationassay (MVD), mice treated with 30 mpk of 2 failed to show any signs of the characteristic cutaneous flushing response observed with niacin treatment. This putative decoupling of the free fatty acid and cutaneous flushing effect characteristic of niacin treatment captivated out attention. As a result, pyrazole 2 became the focal point of our medicinal chemistry effort. The initial goal of the program focused on improving the in vitro profile of pyrazole 2. With this goal in mind, we proceeded to explore the SAR around the framework of pyrazole 2. Early in our efforts,we discovered that both the pyrazole and tetrazole moieties were essential in retaining affinity for the receptor. In addition, it was discovered that substituents in either the C4 or C6 positions of the saturated carbon backbone of 2 were poorly tolerated. In light of these observations, we focused our attention around the C5 position of the molecule. Table 1 Agonism of GPR109a by C5substituted pyrazole– tetrazolesa 洛陽理工學院畢業(yè)設計論文 28 Scheme 1. Reaction conditions: (i) LDA, di tbutyl oxalate。 (ii) BnNHNH2–HCl。 (iii) TFA。 (iv) NHS, EDC。 (v) NH4OH。 (vi) cyanuric chloride。 (vii) LDA, Comin’s reagent In order to explore the C5 position of the molecule most judiciously,we utilized triflate 5 as a late stage synthetic intermediate that allowed for the installation of both alkyl and aryl substituents