130049-82-0, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, molecular formula is C11H15ClN2O2, molecular weight is 242.7, as common compound, the synthetic route is as follows.
Example 28.0L of methanol, 1.04 Kg (4.28 moles) of 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-4H- pyrido[l,2-a]pyrimidin-4-one, 1.10 kg (10.89 moles) of triethyl amine and 1.0 kg (3.89 moles) of 6-fluoro-3(4-piperidinyl)-l,2-benzisoxazole hydrochloride were charged. The reaction mass was heated to reflux. The completion of reaction was monitored by HPLC. The reaction mass was cooled to 25-30C and further chilled to 0-5C, stirred for 30 min. and centrifuged. The cake obtained was washed with 0.5 L of chilled methanol. Weight of wet product containing paliperidone and inorganic salts was 1.0 kg, HPLC purity of paliperidone: 98.88%, keto- paliperidone impurity: 0.05%. The wet product obtained was further used for purification process.
Statistics shows that 130049-82-0 is playing an increasingly important role. we look forward to future research findings about 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one.
Reference:
Patent; MEGAFINE PHARMA (P) LTD.; MATHAD, Vijayavitthal Thippannachar; SOLANKI, Pavankumar Vrajlal; SEKHAR, Babu Uppelli; PANDIT, Bhushan Sudhakar; WO2012/35554; (2012); A1;,
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