181525-38-2Relevant articles and documents
A blue-emitting organic compound 9-hydroxyl-3-hydroxyethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one: Synthesis, crystal structure and luminescent properties
Zhang, Huaihong,Sun, Yu,Chen, Xiaodan,Li, Chao,Sun, Baiwang
, p. 464 - 469 (2010)
A blue-emitting organic compound, 9-hydroxyl-3-hydroxyethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (I), was synthesized by the reaction of 2-amino-3-hydroxylpridine with 2-acetylbutyrolactone. The crystal of the title compound in larger size was reported for the first time through the slow evaporation method. The whole molecule in the crystal is non-planar, but the two conjugated rings are almost co-planar (with an average dihedral angle of only about 1.621°). The hydroxyl group is in trans position to the pyrido[1,2-a]pyrimidin heterocyclic moiety. The molecules are linked by the N-H?O, O-H?O and C-H?O hydrogen bonds into two-dimensional sheets. Additionally, the π-π interactions (average distance 3.3680 A?) interconnect the sheets stabilizing the crystal structure. At room temperature, the compound exhibits an intense blue emission at 432 nm upon 323 nm excitation in the solid state. The simple EL device with the configuration of ITO/I + PMMA/Ag was fabricated, where the compound (I) was used as a main emitting material. The EL device fabricated had a maximum brightness of 289 cd m-2. The thermal stability of the compound was also investigated by thermogravimetric analysis (TGA).
PROCESS FOR PREPARING PALIPERIDONE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
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Page/Page column 13, (2011/07/07)
The present invention discloses the process for the preparation of paliperidone and its pharmaceutically acceptable salts comprising (a) condensing 2-amino-3-hydroxy- pyridine with 2-acetylbutyro lactone in the presence of an acid catalyst to isolate 9- hydroxy-3-(2-hydroxyethyl)-2-rnethyl-4H-pyrido[l, 2-a] pyrimidin-4-one; treating 9- hydroxy-3-(2-hydroxyethyl)-2-methyl-4H-pyrido[l, 2-a] pyrimidin-4-one with a chlorinating agent; hydrogenating the product in the presence of one or more lewis acids to obtain 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[l,2-a]- pyrimidin-4-one; and condensing3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2- methyl-4H-pyrrido[l,2-a]-pyrimidin-4-one. The present invention also discloses processes for the preparation of intermediates useful in the preparation of paliperidone and its pharmaceutically acceptable salts.
PREPARATION OF 9-HYDROXY-3- (2-HYDROXYETHYL) -2-METHYL-4H-PYRID0[1, 2-a] PYRIMIDIN-4-ONE AND CRYSTALS THEREOF
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Page/Page column 5; 6, (2008/06/13)
The present invention concerns a process for preparing crystalline 3-(2-chloro-ethyl)-9-hydroxy-2-methyl-4H-pyrido[1 ,2-a]pyrimidin-4-one substantially free of 2-acetylbutyrolactone.
