- Synthesis of tetrazolopiperazine building blocks by a novel multi-component reaction
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A novel Ugi-five-centre-four-component reaction (U-5C-4CR) of aldehydes, primary amines, trimethylsilylazide and 2-isocyanoethyltosylate yielding tetrazolopiperazine building blocks is described.
- Umkehrer, Michael,Kolb, Jürgen,Burdack, Christoph,Ross, Günther,Hiller, Wolfgang
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- One-Pot Synthesis of Cyclic Isothioureas
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The one-pot synthesis of cyclic isothioureas is reported. This method provides a straightforward and efficient approach to the synthesis of a broad range of cyclic isothioureas with yields of up to 90% and in quantities of up to 5 g. It is of great value for the preparation of classic organocatalysts, such as benzotetramisole and homobenzotetramisole.
- Wang, Jun,Sun, Zhihua
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supporting information
p. 1751 - 1756
(2021/08/27)
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- TETRAHYDRO-TETRAZOLO[1,5-A]PYRAZINES AS ROR-GAMMA INHIBITORS
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The present invention relates to tetrahydro-tetrazolo[l,5-a]pyrazine compounds of formula (I), wherein R1 denotes -R3, -CH2-R3 or -CO-R3; R2 denotes Ar2, Hetar2 or C3-7-cycloalkyl; and R3 denotes Ar3, Hetar3 or C3-7-cycloalkyl. These compounds are useful for inhibiting the retinoid-related orphan receptor γ (ROR γ, ROR-gamma) and for the prevention and/or treatment of medical conditions affected by ROR γ activity such as rheumatoid arthritis, multiple sclerosis, psoriasis, ulcerative colitis, asthma, autoimmune hepatitis or type 1 and type 2 diabetes.
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Page/Page column 50; 51
(2015/07/07)
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