IP Library Granted Patent US 9,695,130
Granted Patent B2
US 9,695,130 · App. 15/116,861 · Granted Jul 4, 2017

Rosuvastatin calcium and process for producing intermediate thereof

Inventors: Naoyuki Watanabe (Fukuoka, JP); Masaki Nagahama (Fukuoka, JP); Takashi Ohtani (Kanagawa, JP)
Assignee: API CORPORATION
C07D239/42C12N9/0006C12P17/12
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Quick Facts
Patent No.
US 9,695,130
App. No.
15/116,861
Granted
Jul 4, 2017
Kind
B2
Abstract

An object of the present invention is to provide a novel method capable of producing rosuvastatin calcium and intermediates therefor efficiently, inexpensively and with high purity. The present invention provides a method of efficiently producing rosuvastatin calcium and intermediates therefor having a high purity at an industrial scale, without using an extremely low temperature reaction or a special asymmetric catalyst.

Claims (9)

1. A production method of rosuvastatin calcium, comprising (B) a step of converting a compound represented by the following formula (12):

wherein M is an alkali metal element, an alkaline earth metal element or hydrogen, to a compound represented by the following formula (13):

2. The production method according to claim 1 , comprising, prior to said step (B), (Aa) a step of converting a mixture of a compound represented by the following formula (14):

wherein R is a primary alkyl group having 1-8 carbon atoms or a secondary alkyl group having 3-6 carbon atoms, and a compound represented by the following formula (15):

wherein R is as defined above, to a mixture of a compound represented by the following formula (16):

wherein M is an alkali metal element, an alkaline earth metal element or hydrogen, and a compound represented by said formula (12), by hydrolyzing same in the presence of a base.

3. A purification method of rosuvastatin calcium comprising a compound represented by the following formula (12):

wherein M is an alkali metal element, an alkaline earth metal element or hydrogen, comprising (B) a step of converting the compound represented by the formula (12) to a compound represented by the following formula (13):

4. Rosuvastatin calcium comprising not less than 1 ppm and not more than 1000 ppm of a compound represented by the following formula (13):

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 19, 2016
From: WATANABE, NAOYUKI; DEKISHIMA, YASUMASA; NAGAHAMA, MASAKI; MAEDA, TOMOKO; OHTANI, TAKASHI; ITO, KOSUKE; KAWABATA, HIROSHI
To: API CORPORATION
Reel/Frame 040066/0202 →
Priority Claims (3)
JP 2014-021769 · Feb 6, 2014 · national
JP 2014-209142 · Oct 10, 2014 · national
JP 2014-209480 · Oct 10, 2014 · national
Continuity (1)
Related Publication 20160347718A1 · Dec 1, 2016