63234-80-0Relevant articles and documents
A method for preparing risperidone chloro
-
Paragraph 0033; 0035; 0036; 0038; 0039; 0041; 0046; 0048, (2019/05/15)
The invention discloses a method for preparing risperidone chloro, the risperidone [...] shown in structural formula II, the method comprises the following steps: a) the 2 - aminopyridine, α - acetyl - γ - butyrolactone in toluene is added, after mixing, drop added to the phosphorus oxychloride or phosphorus oxychloride in toluene solution, during the dropping control phosphorus oxychloride at a temperature between 75 - 110 °C, the completion of the dropping, thermal insulation obtained through the reaction of intermediate III 2 - methyl - 3 - (2 - chloro ethyl) - pyrido [1, 2 - a] pyrimidine - 4 - one; b) in the step a) the obtained intermediate III 2 - methyl - 3 - (2 - chloro ethyl) - pyrido [1, 2 - a] pyrimidine - 4 - one is dissolved in hydrochloric acid solution, adding palladium-carbon, the pressure of 0.20 ± 0.05 mpa the hydrogenation is carried out under the conditions of the reaction, the solution is neutralized, extraction to obtain 2 - methyl - 3 - (2 - chloroethyl) - 6, 7, 8, 9 - tetrahydro-pyrido [1, 2 - a] pyrimidine - 4 - one. The method by changing the way the reaction material, and thereby the conversion, the intermediate (III) of the yield can be up to 80 - 85%; optimize the post treatment process, and is favorable for industrial production.
Preparation of 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one, a Key Intermediate for the Synthesis of Paliperidone
Solanki, Pavankumar V.,Uppelli, Sekhar Babu,Sarode, Ganesh G.,Kardile, Pritesh B.,Bembalkarb, Saroj R.,Mathad, Vijayavitthal T.
, p. 296 - 302 (2016/07/06)
-
Synthesis of 2-methyl-3-(2-(piperazin-1-yl)ethyl)-6,7,8,9-tetrahydro- 4hpyrido[1,2-a]pyrimidin-4-one derivatives as antimicrobial agents
Krishnamurthy, Byregowda,Vinaya, Kambappa,Prasanna, Doddakunche S.,Raghava, Byregowda,Rangappa, Kanchugarakoppal S.
, p. 988 - 995 (2012/07/01)
A series of novel 2-methyl-3-(2-(piperazin-1-yl)ethyl)-6,7,8,9-tetrahydro- 4H-pyrido[1,2-a]pyrimidin-4-one sulfonamide and carboxamide derivatives were synthesized in good yield. The synthesized compounds were characterized by 1H-NMR, FTIR and elemental analysis. All the synthesised compounds were screened for their in vitro antimicrobial activity by agar well diffusion and micro dilution method against standard strains of Gram-positive (Bacillus subtilis MTCC 121, Staphylococcus epidermidis 435), and Gram-negative (Xanthomonas campestris 7903 and Pseudomonas aeruginosa MTCC 7908) bacteria. Compound 7a and compound 8d with dichloro substitution among sulphonamide and carboxamide series respectively showed potent inhibitory activity.