- Design and synthesis of 5-chloro-2-hydroxy-3-triazolylbenzoic acids as HIV integrase inhibitors
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A series of potential HIV-1 integrase inhibitors based on 5-chloro-2-hydroxy-3-triazolylbenzoic acid scaffold was designed and synthesized. Some of these compounds exhibit potent inhibitory activities at micromolar concentrations against HIV-1 integrase i
- Chen, Jie,Liu, Cheng-Fu,Yang, Cheng-Wen,Zeng, Cheng-Chu,Liu, Wei,Hu, Li-Ming
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- 3-process for the preparation of amino-salicylic acid
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The invention relates to a novel preparation method of 3-aminosalicylic acid. The novel preparation method is characterized in that a salicylic acid compound I as an initial raw material having a general formula shown in the description and a nitration agent undergo a reaction to produce a 3-nitrosalicylic acid compound II having a general formula shown in the description, and the 3-nitrosalicylic acid compound II undergoes nitryl catalytic hydrogenation reduction and dehalogenation hydrogenolysis reactions in the presence of an effective dose of a catalyst and hydrogen donors so that 3-aminosalicylic acid is produced.
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Paragraph 0024-0026
(2016/10/08)
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- Development of a Phase-Transfer-Catalyzed, [2,3]-Wittig Rearrangement
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An investigation into the use of phase-transfer catalysis for the [2,3]-sigmatropic rearrangement of allyloxy carbonyl compounds is described. Initial studies focused on identifying viable substrate classes that would undergo selective [2,3]-rearrangement under phase-transfer catalysis. Under certain conditions, the [2,3]-sigmatropic rearrangement of allyloxy carbonyl compounds takes place in the presence of a phase-transfer agent, providing a rare example of a phase-transfer-catalyzed unimolecular reaction. In the course of this investigation, it was found that catalysis is dependent on several variables including base concentration, catalyst structure, and substrate lipophilicity. Preliminary testing of chiral, nonracemic phase-transfer catalysts has shown promising levels of enantioselectivity for future development.
- Denmark, Scott E.,Cullen, Lindsey R.
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p. 11818 - 11848
(2015/12/11)
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- Fungicidal compositions and methods, and compounds and methods for the preparation thereof
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Fungicidal compositions and methods comprising acylated aminosalicylamides (AASA) described herein. Novel cyclic amines and 3-nitrosalicylamides, and their use as pesticides and in the preparation of the antifungal AASA compounds are also disclosed.
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- Synthesis and Enzymatic Evaluation of Conformationally Defined Carnitine Analogs
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Carnitine (1, 3-hydroxy-4-trimethylammoniobutyrate) is essential as a donor and acceptor of acyl groups in cellular metabolism.The major solution conformation of carnitine about C3-C4 contains the gauche reletionship between the trimethylammonium and hydr
- Brouillette, Wayne J.,Saeed, Ashraf,Abuelyaman, Ahmed,Hutchison, Tracy L.,Wolkowicz, Paul E.,McMillin, Jeanie B.
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p. 4297 - 4303
(2007/10/02)
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