- Catalytic Aerobic Dehydrogenatin of N-Heterocycles by N-Hydoxyphthalimide
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Catalytic methods for the aerobic dehydrogenation of N-heterocycles are reported. In most cases, indoles are accessed efficiently from indolines using catalytic N-hydroxyphthalimide (NHPI) as the sole additive under air. Further studies revealed an improved catalytic system of NHPI and copper for the preparation of other heteroaromatics, for example quinolines. (Figure presented.).
- Chen, Weidong,Tang, Hao,Wang, Weilin,Fu, Qiang,Luo, Junfei
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supporting information
p. 3905 - 3911
(2020/08/10)
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- Method for preparing indole compound through air oxidation catalyzed by N-hydroxyphthalimide
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The invention discloses a method for preparing an indole compound through non-transition metal catalyzed air oxidation. According to the method, the low-cost N-hydroxyphthalimide is used as a catalystand air is used as an oxidizing agent, wherein indoline compounds are oxidized in an organic solvent, and synthesis of the indoline compounds is achieved. The method has the advantages of simple reaction operation, low reaction cost, high yield, mild conditions, no heavy metal pollution and the like.
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Paragraph 0077-0079
(2020/11/23)
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- Electrosynthesis of Dihydropyrano[4,3-b]indoles Based on a Double Oxidative [3+3] Cycloaddition
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Oxidative [3+3] cycloadditions offer an efficient route for six-membered-ring formation. This approach has been realized based on an electrochemical oxidative coupling of indoles/enamines with active methylene compounds followed by tandem 6π-electrocyclization leading to the synthesis of dihydropyrano[4,3-b]indoles and 2,3-dihydrofurans. The radical–radical cross-coupling of the radical species generated by anodic oxidation combined with the cathodic generation of the base from O2 allows for mild reaction conditions for the synthesis of structurally complex heterocycles.
- Choi, Subin,Park, Cheol-Min,Park, Jinhwi,Sim, Jeongwoo,Yu, Eunsoo
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supporting information
p. 11886 - 11891
(2020/05/22)
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- Azacycle diketone compound and preparation method thereof (by machine translation)
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The invention provides a azacyclodiketone compound which is characterized by being a compound represented by the following structure. The compound has inhibitory activity on cap-dependent endonuclease. (by machine translation)
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Paragraph 0827-0833
(2020/09/12)
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- Detosylative (Deutero)alkylation of Indoles and Phenols with (Deutero)alkoxides
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An efficient strategy for N/O-(deutero)alkylation of indoles and phenols with alkoxides/alcohols as the alkylation reagents is described. The consecutive detosylation/alkylation transformations feature mild reaction conditions, high ipso-selectivity, and good functional group tolerance (>50 examples). A one-pot selective N-alkylation of unprotected indoles with alcohols and TsCl is also realized. The application of this method is demonstrated by the introduction of isotope-labeled (CD3 and 13CH3) groups using the readily accessible labeled alcohols and the synthesis of pharmaceuticals.
- Zhu, Ming-Hui,Yu, Cheng-Long,Feng, Ya-Lan,Usman, Muhammad,Zhong, Dayou,Wang, Xin,Nesnas, Nasri,Liu, Wen-Bo
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supporting information
p. 7073 - 7077
(2019/09/30)
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- AMINOACYLINDAZOLE IMMUNOMODULATORS FOR TREATMENT OF AUTOIMMUNE DISEASES
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2-Acylindazole compounds of formula I or formula II are disclosed. These compounds inhibit Coagulation Factor XIIa. They are useful to treat autoimmune diseases.
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Paragraph 78
(2017/12/29)
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- 5-HT3 RECEPTOR MODULATORS, METHODS OF MAKING, AND USE THEREOF
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Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of maki
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Page/Page column 17
(2009/12/23)
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- Synthesis of highly substituted indole alkaloid species via [4+1] cyclization of nucleophilic carbenes and indole isocyanates
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Thermally induced [4+1] cyclization between indole isocyanates and dimethoxycarbene or bis(propylthio)carbene has been achieved with good chemical efficiency. The methodology provides rapid access to fused pyrroloindole substructures commonly found in a variety of indole alkaloid natural products.
- Rigby, James H.,Burke, Patrick J.
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p. 643 - 653
(2007/10/03)
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- Synthesis and biological activity of N-(aminoiminomethyl)-1H-indole carboxamide derivatives as Na+/H+ exchanger inhibitors
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A series of N-(aminoiminomethyl)-1H-indole carboxamide derivatives were synthesized and their inhibitory potencies against the Na+/H+ exchanger were measured. Variation of the carbonylguanidine group at the 2- to 7- position of the indole ring system showed that a substitution at the 2- position improved the Na+/H+ exchanger inhibitory activity the most in vitro. This led to the synthesis and evaluation of an extensive series of N- (aminoiminomethyl)-1H-indole-2-carboxamide derivatives. Derivatives having an alkyl or substituted alkyl group at the 1-position of the indole ring system showed higher levels of in vitro activities. N-(aminoiminomethyl)-1-(2- phenylethyl)-1H-indole-2-carboxamide (49) had the strongest activity.
- Kitano, Masafumi,Kojima, Atsuyuki,Nakano, Kazuhiro,Miyagishi, Akira,Noguchi, Tsuyoshi,Ohashi, Naohito
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p. 1538 - 1548
(2007/10/03)
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