- Nickel-Catalyzed Reversible Functional Group Metathesis between Aryl Nitriles and Aryl Thioethers
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We describe a new functional group metathesis between aryl nitriles and aryl thioethers. The catalytic system nickel/dcype is essential to achieve this fully reversible transformation in good to excellent yields. Furthermore, the cyanide- and thiol-free reaction shows high functional group tolerance and great efficiency for the late-stage derivatization of commercial molecules. Finally, synthetic applications demonstrate its versatility and utility in multistep synthesis.
- Delcaillau, Tristan,Boehm, Philip,Morandi, Bill
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supporting information
p. 3723 - 3728
(2021/04/07)
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- Synthesis method of 3-aminoazetidine
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The invention belongs to the technical field of organic synthesis, and specifically relates to a synthesis method of 3-aminoazetidine. The method comprises the following steps: performing sulfonationreaction in acetonitrile by taking 1-benzyl-3-acridine b
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Paragraph 0023; 0026-0028; 0032-0034
(2019/04/04)
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- DERIVATIVES OF 6-(2,3-DICHLOROPHENYL)-1,2,4-TRIAZIN-5- AMINE
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The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.
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Paragraph 0474
(2015/07/07)
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- Influence of ring size on the cognition-enhancing activity of DM235 and MN19, two potent nootropic drugs
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A series of analogs of DM235 and MN19, characterized by rings with different size, have been prepared and evaluated for their nootropic activity in the mouse passive-avoidance test. It was found that the optimal ring size for the analogs of DM235, showing endocyclic both amidic groups, is 6 or 7 atoms. For the compounds structurally related to MN19, carrying an exocyclic amide group, the piperidine ring is the moiety which gives the most interesting compounds.
- Guandalini,Martini,Di Cesare Mannelli,Dei,Manetti,Scapecchi,Teodori,Ghelardini,Romanelli
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supporting information; experimental part
p. 1936 - 1939
(2012/04/04)
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- A practical and facile synthesis of azetidine derivatives for oral carbapenem, L-084
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An orally active carbapenem L-084, which exhibits high bioavailability in humans, has a 1-(1,3-thiazolin-2-yl)azetidin-3-ylthio moiety at the C-2 position of the 1β-methylcarbapenem skeleton. We established a practical and cost-effective synthesis of 3-mercapto-1-(1,3-thiazolin-2-yl)azetidine (1) for further scale-up production of L-084. This synthesis method entails an industry-oriented reaction of azetidine ring-closure to yield N-benzyl-3-hydroxyazetidine (16), which is eventually converted to 1 via key intermediates, Bunte salts 19 and 20.
- Isoda, Takeshi,Yamamura, Itsuki,Tamai, Satoshi,Kumagai, Toshio,Nagao, Yoshimitsu
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p. 1408 - 1411
(2007/10/03)
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