US 11,814,355 B2
Method for synthesizing pitavastatin t-butyl ester
Huan Huang, Hefei (CN); Kai Li, Hefei (CN); Qingyun Huang, Hefei (CN); Fuming Zhan, Hefei (CN); and Qingguo Huang, Hefei (CN)
Filed by Anhui Qingyun Pharmaceutical and Chemical Co., Ltd., Hefei (CN)
Filed on Feb. 10, 2021, as Appl. No. 17/173,171.
Claims priority of application No. 202010783672.X (CN), filed on Aug. 6, 2020.
Prior Publication US 2022/0041556 A1, Feb. 10, 2022
Int. Cl. C07D 215/14 (2006.01); B01J 31/12 (2006.01); B01J 27/24 (2006.01); B01J 23/30 (2006.01); B01J 27/232 (2006.01)
CPC C07D 215/14 (2013.01) [B01J 23/30 (2013.01); B01J 27/232 (2013.01); B01J 27/24 (2013.01); B01J 31/121 (2013.01); B01J 31/122 (2013.01); B01J 31/128 (2013.01); B01J 2531/11 (2013.01); B01J 2531/12 (2013.01)] 28 Claims
 
1. A method for synthesizing pitavastatin t-butyl ester, comprising the steps of:
(a) obtaining a substance B through reacting (4R-CIS)-6-chloromethyl-2,2-dimethyl-1,3-dioxolane-4-acetic acid tert-butyl ester with a substance A under an action of a first base catalyst;
(b) oxidizing with an oxidizing agent to obtain a substance C;
(c) reacting with 2-cyclopropyl-4-(4-fluorophenyl)-quinoline-3-formaldehyde under an action of a second base catalyst to obtain a substance D; and
(d) carrying out an acid deprotection to obtain pitavastatin t-butyl ester, wherein a structural formula of said substance A, said substance B, said substance C, said substance D, and said pitavastatin t-butyl ester is as follows:

OG Complex Work Unit Chemistry
R is one of hydrogen, alkyl, cycloalkyl, phenyl, and substituted phenyl.