Preparation method for rosuvastatin calcium intermediate

• Main Authors: QIAO ZAIYIN, LU CHENGXIAN, TU LIANG, JI JIAN, TIAN JIANHONG, DENG PENG
• Format: Patent
• Language: English
• Published: 16.09.2015
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The application provides a preparation method for a rosuvastatin calcium intermediate. The method comprises the following steps: a, condensation reaction: a step of adding a main chain Z8 and a side chain J6 into a mixed solution of toluene and acetonitrile, then adding 4-butylammonium bromide, carrying out heating and pressure-reduced concentration so as to obtain a crude H1 product; b, purification of a condensation product: a step of adding a mixture of n-hexane and petroleum ether, and carrying out heating, cooling, heating, filtering and pressure-reduced distillation so as to obtain a H1 product; c, deprotection reaction: a step of adding the H1 product into acetonitrile, then adding an acid-acetonitrile solution under ice bath, after completion of the reaction, controlling a pH value to 7 to 9, then separating the obtained solution and washing an organic layer, further separating the solution and adding a drying agent into the organic layer, then carrying out filtering and pressure-reduced concentration so as to obtain an oily substance, and adding tetrahydrofuran for crystallization so as to obtain an crude H2 product; and d, purification of a deprotection product: a step of adding acetone and tetrahydrofuran, after dissolving, adding activated carbon, and carrying out stirring, hot filtration, cooling, crystallization, filtering and vacuum drying so as to obtain a final H2 product. By using the preparation method for the rosuvastatin calcium intermediate provided by the invention, yield and purity are high, and cost is low.