- Rapid and efficient synthesis of stable isotope labeled [ 13C4, D4]-5-(hydroxymethyl)thiazole: Versatile building block for biologically interesting compounds
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5-(Hydroxymethyl)thiazole is a versatile building block for many biologically active compounds. A rapid and efficient four- step synthesis of its stable isotope labeled counterpart with four 13C and four deuterium atoms in 32% total yield is reported. Condensation of [13C 2]-chloro acetic acid with [13C]-thiourea gave [ 13C3]-2,4-thiazolidinedione. Reaction of [ 13C3]-2,4-thiazolidinedione with phosphorus oxybromide and [13C, D]-DMF (Me2N13CDO) produced [ 13C4 D]-2,4-dibromo- thiazole-5-carboxaldehyde. The resultant aldehyde was then reduced by sodium borodeuteride to [ 13C4, D2]-(2,4-dibromo- thiazol-5-yl)-methanol. Catalytic deuteration of [13C4, D2]-(2,4- dibromo-thiazol-5-yl)-methanol by palladium black with deuterium gas at 1 atm pressure and room temperature produced completely de-brominated [ 13C4, D4]-5-(hydro- xymethyl)thiazole. De-bromination of the 2,4-dibromothiazole by the catalysis of palladium black provides a simple and convenient synthetic method for the stable isotope labeled and potentially radioactive isotope labeled thiazole compounds. Copyright
- Lin, Ronghui,Salter, Rhys,Gong, Yong
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- 2-(1-HETEROARYLPIPERAZIN-4-YL)METHYL-1,4-BENZODIOXANE DERIVATIVES AS ALPHA2C ANTAGONISTS
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Compounds of formula I (formula I), wherein A is an optionally substituted five-membered unsaturated heterocyclic ring containing 1, 2 or 3 N, O or S ring heteroatom(s) exhibit alpha2C antagonistic activity and are thus useful for the treatment of diseases or conditions of the peripheric or central nervous system.
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(2016/12/22)
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- Pyrrolopyrimidines as therapeutic agents
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Chemical compounds having structural formula I and physiologically acceptable salts and metabolites thereof, are inhibitors of serine/threonine and tyrosine kinase activity. Several of the kinases, whose activity is inhibited by these chemical compounds, are involved in immunologic, hyperproliferative, or angiogenic processes. Thus, these chemical compounds can ameliorate disease states where angiogenesis or endothelial cell hyperproliferation is a factor. These compounds can be used to treat cancer and hyper proliferative disorders, rheumatiod arthritis, disorders of the immune system, trasplant refections and imflammatory disorders.
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