57401-76-0Relevant articles and documents
Simple preparation method of 2-aminopyrimidine-5-formate
-
, (2020/01/25)
The invention provides a simple preparation method of 2-aminopyrimidine-5-formate. The preparation method comprises: carrying out a substitution reaction on 2-methacrylate as a raw material and a halogenating reagent 1, carrying out an addition reaction with a halogenating reagent 2 to obtain 2,3,3-trihalogenated-2-halogenated methyl propionate, and condensing the obtained 2,3,3-trihalogenated-2-halogenated methyl propionate and a guanidine salt to prepare 2-aminopyrimidine-5-formate. According to the invention, the raw materials used in the method are cheap, easy to obtain and low in cost; and the preparation method has characteristics of simpleness, easily achieved conditions, good operation safety, little wastewater generation, environmental protection, high target product yield and high target product purity, and is suitable for industrial production.
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
-
Paragraph 1024, (2013/04/10)
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.
Retinoidal pyrimidinecarboxylic acids. Unexpected diaza-substituent effects in retinobenzoic acids
Ohta, Kiminori,Kawachi, Emiko,Inoue, Noriko,Fukasawa, Hiroshi,Hashimoto, Yuichi,Itai, Akiko,Kagechika, Hiroyuki
, p. 1504 - 1513 (2007/10/03)
Several pyridine- and pyrimidine-carboxylic acids were synthesized as ligand candidates for retinoid nuclear receptors, retinoic acid receptors (RARs) and retinoic X receptors (RXRs). Although the pyridine derivatives, 6-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]pyridine- 3-carboxylic acid (2b) and 6-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carboxamido]pyridin e-3-carboxylic acid (5b) are more potent than the corresponding benzoic acid-type retinoids, Am80 (2a) and Am580 (5a), the replacement of the benzene ring of Am580 (5a), Am555 (6a), or Am55 (7a) with a pyrimidine ring caused loss of the retinoidal activity both in HL-60 cell differentiation assay and in RAR transactivation assay using COS-1 cells. On the other hand, pyrimidine analogs (PA series, 10 and 11) of potent RXR agonists (retinoid synergists) with a diphenylamine skeleton (DA series, 8 and 9) exhibited potent retinoid synergistic activity in HL-60 cell differentiation assay and activated RXRs. Among the synthesized compounds, 2-[N-n-propyl-N-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)amino] pyrimidine-5-carboxylic acid (PA013, 10e) is most active retinoid synergist in HL-60 assay.