15908-64-2Relevant academic research and scientific papers
A Novel One-Pot Method for the Synthesis of Pyrimidine Derivatives Using Ketene N,S-Acetal with Aryl Aldehydes
Hagimori, Masayori,Murakami, Yuka,Mizuyama, Naoko,Tominaga, Yoshinori
, p. 197 - 201 (2016/02/10)
(Chemical Equation Presented) A very simple and facile one-pot method for the synthesis of pyrimidine derivatives is presented. In this method, 2-aryl-pyrimidine derivatives were prepared by the reaction of ketene N,S-acetal 1 with commercially available aryl aldehydes by heating under solvent and catalyst-free conditions. The synthesized pyrimidine derivatives showed blue-green fluorescence in solid state.
A convenient synthesis of pyrimidinone and pyrimidine containing bisheteroarenes and analogs
Maurya, Hardesh K.,Gupta, Atul
, p. 22106 - 22114 (2014/06/23)
The synthesis of pyrimidinone containing bisheteroarenes (3) and related analogs (9 and 10) by the reaction of active methylenes or substituted methyl acrylate with nitrogen containing precursors viz. amidines, or thiourea in water as well as other organic solvents was studied. Synthesized compounds have further been explored for the synthesis of diversified pyrimidines 4, 6-8, 11, 12 and 14 through a sequential approach. This journal is the Partner Organisations 2014.
Synthesis and biological evaluation of 5-carbamoyl-2-phenylpyrimidine derivatives as novel and potent PDE4 inhibitors
Goto, Taiji,Shiina, Akiko,Yoshino, Toshiharu,Mizukami, Kiyoshi,Hirahara, Kazuki,Suzuki, Osamu,Sogawa, Yoshitaka,Takahashi, Tomoko,Mikkaichi, Tsuyoshi,Nakao, Naoki,Takahashi, Mizuki,Hasegawa, Masashi,Sasaki, Shigeki
, p. 7025 - 7037 (2013/11/06)
5-Carbamoyl-2-phenylpyrimidine derivative 2 has been identified as a phosphodiesterase 4 (PDE4) inhibitor with moderate PDE4B inhibitory activity (IC50 = 200 nM). Modification of the carboxylic acid moiety of 2 gave N-neopentylacetamide derivative 10f, which had high in vitro PDE4B inhibitory activity (IC50 = 8.3 nM) and in vivo efficacy against lipopolysaccharide (LPS)-induced pulmonary neutrophilia in mice (ID50 = 16 mg/kg, ip). Furthermore, based on the X-ray crystallography of 10f bound to the human PDE4B catalytic domain, we designed 7,8-dihydro-6H-pyrido[4,3-d] pyrimidin-5-one derivative 39 which has a fused bicyclic lactam scaffold. Compound 39 exhibited excellent inhibitory activity against LPS-induced tumor necrosis factor alpha (TNF-α) production in mouse splenocytes (IC 50 = 0.21 nM) and in vivo anti-inflammatory activity against LPS-induced pulmonary neutrophilia in mice (41% inhibition at a dose of 1.0 mg/kg, i.t.).
Microwave-assisted solvent-free synthesis of highly functionalized pyrimidine derivatives
Yan, Shengjiao,Niu, Yanfei,Chen, Xuebing,Liu, Yongjiang,Lin, Jun
, p. 877 - 882 (2012/10/30)
We here described an efficient method for the synthesis of a series of highly functionalized pyrimidines via the addition and condensation reaction of ketene dithioacetals with guanidine carbonate or amidine hydrochlorides by microwave irradiation under s
New heterocyclic compounds
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Page/Page column 10, (2008/12/08)
Provided herein are heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and compositions, metabolites and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as described herein. Further described herein in particular are heterocyclic compounds of the formula (I) for treating various diseases. and disorders by administering in a patient one or more TNF-α, Thromboxane synthase, 5-LOX, and PDE4 inhibitors. In particular described herein are methods for treating immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; ischemic heart disease; atherosclerosis; cancer; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; cachexia; asthma; bone resorption diseases; ischemia reperfusion injury; brain trauma; multiple sclerosis; sepsis; septic shock; toxic shock syndrome; fever, and myalgias due to infection and diseases mediated by HIV-1; HIV-2; HIV-3; cytomegalovirus (CMV); influenza; adenovirus; the herpes viruses (including HSV-1, HSV-2) and herpes zoster viruses in a mammal comprising administering an effective amount of a compound of formula (I).
Suitably functionalised pyrimidines as potential antimycotic agents
Agarwal, Nidhi,Raghuwanshi, Sandeep K.,Upadhyay,Shukla,Ram, Vishnu J.
, p. 703 - 706 (2007/10/03)
Various suitably functionalised pyrimidine derivatives have been synthesized to explore their potential as antimycotic agents. Some of the synthesized compounds 4c, 4d, 8a-e have shown highly significant in vitro antifungal activity against five human pathogenic fungi. (C) 2000 Elsevier Science Ltd. All rights reserved.
Chemotherapeutic agents: Part XXIII - Synthesis of π-deficient pyrimidines and fused pyrimidines as leishmanicides
Ram, Vishnu J,Haque, Navedul,Nath, Mahendra
, p. 754 - 759 (2007/10/02)
Various ?-deficient pyrimidines and fused purimidines have been synthesized and evaluated for their leishmanicidal activity against L. donovani.
REACTION OF KETENE DITHIOACETALS WITH THIOAMIDES. A SYNTHESIS OF PYRIMIDINE DERIVATIVES
Lorente, Antonio,Garcia, M. Luisa,Fernandez, Misericordia,Soto, Jose L.
, p. 1573 - 1582 (2007/10/02)
Reaction of ketene dithioacetals with thioamides gave 5-cyano-2-methyl(or phenyl)-6-methylthio-4-thioxopyrimidines.
