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TAbstract: The rapid development of the economy and society and the coordinated advancement of industrialization and urbanization have led to the intensification of the man-land contradiction. It requires the use of spatial multi-functionality to maximize the value of regional space, promote the diversification of social needs, and help rural areas meet multi-functional needs. Correct identification of rural regional functions is an important way to implement the strategy of rural revitalization and comprehensively deepen rural reform. Taking Sichuan Province as the research subject, we constructed a multi-functional evaluation index system for rural areas from four perspectives, that is, economic development, food production, social security, and ecological protection. We used the comprehensive evaluation method to investigate the spatial distribution characteristics of various functions, and the vertical and horizontal comparison method to identify the dominant function and short board function, and the regional types were divided accordingly. In cognizance of the five major economic zones in Sichuan Province, this paper puts forward corresponding rural revitalization paths of various regional types to provide a benchmark for the implementation of a rural revitalization strategy in Sichuan Province. A clear spatial pattern differentiation of the rural regional function in Sichuan Province was noted. The regional characteristics of the economic development function and the social security function are the same, showing a gradual weakening differentiation pattern from southeast to northwest Sichuan. The spatial agglomeration characteristics of the grain production function in the Chengdu Plain Economic Zone and the Anning River Basin in Panxi are obvious, and the ecological conservation function is gradually enhanced from southeast to northwest Sichuan. Via the identification of the dominant function and the short board function, we divided Sichuan Province into three categories: dominant development type, polarization development type, and comprehensive development type. Among them, the dominant development type and the polarization development type were divided into nine sub-categories according to their characteristics. The specific implementation paths of rural revitalization are proposed according to different regional types, in which the dominant development type gives priority to playing the dominant function while integrating and coordinating other functions to promote comprehensive rural revitalization development. While giving full play to its advantages, the polarization development type complements the shortcomings and achieves basic balanced development. Based on the existing foundation, the comprehensive development model realizes industrial upgrading and becomes the leading means of demonstration of rural revitalization and development in Sichuan Province. The main contribution of this paper is therefore the consolidation of the convergence of poverty alleviation and rural revitalization. The dominant function and short board function are used to classify the regional functions of rural areas in Sichuan Province. The division results are consistent with the regional differentiation of nature and economy in Sichuan Province from different perspectives. The development path of rural revitalization provided decision-making reference for this regional type.

Ergolines were recently identified as a novel class of H3 receptor (H3R) inverse agonists. Although their optimization led to drug candidates with encouraging properties for the treatment of narcolepsy, brain penetration remained low. To overcome this issue, ergoline 1 ((6aR,9R,10aR)-4-(2-(dimethylamino)ethyl)-N-phenyl-9-(pyrrolidine-1-carbonyl)-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinoline-7(4H)-carboxamide)) was transformed into a series of indole derivatives with high H3R affinity. These new molecules were profiled by simultaneous determination of their brain receptor occupancy (RO) levels and pharmacodynamic (PD) effects in mice. These efforts culminated in the discovery of 15 m ((R)-1-isopropyl-5-(1-(2-(2-methylpyrrolidin-1-yl)ethyl)-1H-indol-4-yl)pyridin-2(1H)-one), which has an ideal profile showing a strong correlation of PD effects with RO, and no measurable safety liabilities. Its desirably short duration of action was confirmed by electroencephalography (EEG) measurements in rats.

Ergoline derivative (6aR,9R)-4-(2-(dimethylamino)ethyl)-N-phenyl-9-(pyrrolidine-1-carbonyl)-6,6a,8,9-tetrahydroindolo[4,3-fg]quinoline-7(4H)-carboxamide (1), a CXCR3 antagonist, also inhibits human histamine H3 receptors (H3R) and represents a structurally novel H3R inverse agonist chemotype. It displays favorable pharmacokinetic and in vitro safety profiles, and served as a lead compound in a program to explore ergoline derivatives as potential drug candidates for the treatment of narcolepsy. A key objective of this work was to enhance the safety and efficacy profiles of 1, while minimizing its duration of action to mitigate the episodes of insomnia documented with previously reported clinical candidates during the night following administration. Modifications to the ergoline core at positions 1, 6 and 8 were systematically investigated, and derivative 23 (1-((4aR,8R,9aR)-8-(hydroxymethyl)-1-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)-4,4a,7,8,9,9a-hexahydroindolo[1,14-fg]quinolin-6(1H)-yl)ethanone) was identified as a promising lead compound. Derivative 23 has a desirable pharmacokinetic profile and demonstrated efficacy by enhancing brain concentrations of tele-methylhistamine, a major histamine metabolite. This validates the potential of the ergoline scaffold to serve as a template for the development of H3R inverse agonists.

Papers I-IV (p. 176-210) not available in TEORA due to publisher restrictions Absorption-stripping with aqueous 2-amino-2-methyl-1-propanol (AMP), and especially AMP blends with other amines, such as monoethanolamine (MEA) and piperazine (PZ), presents an attractive option for carbon dioxide (CO2) capture from flue gas in coal-fired power plants. Alkanolamine based solvents degrade in this service. The purpose of this work was to investigate AMP solvent degradation under thermal and oxidizing conditions, to measure rates of degradation for comparison with other solvents, to identify the degradation products and to identify possible degradation pathways. 5 mol/kg AMP without CO2 loading was thermally stable up to 140°C under a blanket gas of N2, exhibiting very low loss rates. However, with an initial CO2 loading of 0.15 and 0.3mol CO2/mol AMP at 135°C, AMP lost 3.8(mol)% and 5.5 (mol)% after 5 weeks, respectively. The steric hindrance in AMP molecule slows down CO2 induced degradation of AMP as compared to MEA, but it does not prevent oxazolidinone formation and oxazolidinone ring-opening into further degradation products. The rate of oxidative degradation of AMP was investigated over a range of temperature, CO2 loading, and AMP concentration. At 100 to 140 °C, degradation was found to be O2 mass transfer limited in the employed batch reactors, however, the degradation rate increased with CO2 loading. No significant effect of pH value was observed on the AMP degradation rate. Acetone, 2,4-lutidine, 4,4-dimethyl-2-oxazolidinone and formate were the main identified degradation products. Oxidative degradation of AMP likely proceeds through a Habstraction step followed by production of a peroxyl radical. The peroxyl radical is proposed to decompose to primary products by intramolecular H-abstraction via a six-membered cyclic transition sate. The reactions of AMP and the primary degradation products lead to the final degradation products. Acetone oxime and 4,4-dimethyl-1,3-oxazolidine were minor products at 100-140°C, but they were major products at 80°C. Temperature significantly affects the distribution of the ultimate degradation products. UV radiation with a medium mercury lamp can dramatically accelerate the oxidation of AMP at 55°C. It seems that UV radiation does not change the primary degradation mechanism of AMP. The degradation products of UV accelerated oxidation are different from those of thermally accelerated oxidation of AMP, probably due to the impact of temperature on the secondary reactions of the primary products. AMP oxidation is proposed to be initiated by a radical mechanism, but the reaction is not a chain reaction. The degradation rate of 1.5 mol/kg PZ is 1.2 mmol/(kg·h) within 19 days, which is approximate half of that of 5 mol/kg AMP under 250 kPa O2 and at 100°C. A possible degradation pathway of PZ is proposed based on the identified products. The degradation rate of AMP in AMP/PZ blends is close to that in a single AMP system, however, PZ degraded faster in the blends than it degraded individually at identical degradation conditions. As compared to degradation of single MEA and AMP solvents, no new product was found in the degraded AMP/MEA mixture without CO2 loading. Increasing the initial MEA concentration in the mixture, the amount of AMP loss decreased indicating that MEA protects AMP from oxidation. This inhibition effect of MEA on AMP degradation could be due to the fact that MEA degrades faster than AMP in the blends.

A novel γ-trifluoroacetylation and a novel ylide-anion formation via conjugated necleophilic addition and their application to the synthesis of trans-γ,δ-unsaturated trifluoromethyl ketones are described.