7185-65-1Relevant academic research and scientific papers
Synthesis of Substituted Aminopyrimidines as Novel Promising Tyrosine Kinase Inhibitors
Stolpovskaya,Kruzhilin,Zorina,Shikhaliev, Kh. S.,Ledeneva,Kosheleva,Vandyshev, D. Yu.
, p. 1322 - 1328 (2019)
A procedure has been proposed for the synthesis of a series of substituted N-(1,3-thiazol-2-yl)-pyrimidin-2-amines and N-(pyrimidin-2-yl)thioureas by reactions of diethyl 2-(ethoxymethylidene)malonate and ethyl 2-(ethyoxymethylidene)-3-oxobutanoate with 1
Method for synthesizing 2-guanidinothiazole compound by one-pot process
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Paragraph 0014, (2020/11/09)
According to the invention, a substituted methyl ketone compound is innovatively used as a raw material, amidinothiourea is added into an alcohol solvent under the conditions of halogeno salt MX and Oxone, and a one-pot process one-step reaction is carried out to obtain the target 2-guanidinothiazole compound. Common methyl ketone is used for replacing an alpha-halogenated carbonyl compound whichis high in price and toxicity, MX which is low in price and easy to obtain is used as a halogen source, the method is novel, raw materials and reagents are cheap, reaction conditions are mild, and operation is easy and convenient, therefore low-cost, convenient and rapid synthesis of the 2-guanidinothiazole compound is achieved.
Identification of potent pyrimidine inhibitors of phosphodiesterase 7 (PDE7) and their ability to inhibit T cell proliferation
Guo, Junqing,Watson, Andrew,Kempson, James,Carlsen, Marianne,Barbosa, Joseph,Stebbins, Karen,Lee, Deborah,Dodd, John,Nadler, Steven G.,McKinnon, Murray,Barrish, Joel,Pitts, William J.
scheme or table, p. 1935 - 1938 (2009/11/30)
A series of pyrimidine based inhibitors of PDE7 are discussed. The synthesis, structure-activity relationships (SAR) and selectivity against several other PDE family members as well as activity in T cells are presented. These compounds were found to have effects on T cell proliferation, however it is not clear whether the mechanism is related to PDE7 inhibition.
Three-component synthesis of 4-aryl-5-cyano-2-hetarylaminopyrimidines
Shikhaliev,Kryl'skaya,Potapov
, p. 1089 - 1090 (2008/02/01)
Three-component condensation of benzooxazol-2-yl-, benzothiazol-2-yl-, and 5-ethoxycarbonyl-4-methyl-1,3-thiazol-2-ylguanidines with orthoesters and aroylacetonitriles afforded 4-aryl-5-cyano-2-hetarylaminopyrimidines.
Fused pyrimidine based inhibitors of phosphodiesterase 7 (PDE7): Synthesis and initial structure-activity relationships
Kempson, James,Pitts, William J.,Barbosa, Joseph,Guo, Junqing,Omotoso, Omonike,Watson, Andrew,Stebbins, Karen,Starling, Gary C.,Dodd, John H.,Barrish, Joel C.,Felix, Raymond,Fischer, Karl
, p. 1829 - 1833 (2007/10/03)
A series of fused pyrimidine based inhibitors of PDE7 have been derived from an earlier screening lead 1. The synthesis, structure-activity relationships (SAR) and selectivity against several other PDE family members are described.
