PROCESS FOR PREPARATION OF CRYSTALLINE [R-(R,R)]-2-(4-FLUOROPHENYL)- ,δ-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1-HEPTANOIC ACID (ATORVASTATIN)

• Main Authors: BRIGGS CHRISTOPHER A, HARASAWA KIKUKO, NAKAGAWA SHINSUKE, MINOHARA KAZUO, WADE ROBERT A, ICHIKAWA HAYASHI, JENNINGS REX ALLEN
• Format: Patent
• Language: English
• Published: 20.03.2014
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide a process for preparation of a stable crystalline form of atorvastatin that is a medicine for treating hyperlipemia and hypercholesterolemia.SOLUTION: The process for the preparation of a crystalline form II or a crystalline form IV of atorvastatin or a hydrate thereof includes (a) a step of suspending a mixture of an amorphous atorvastatin and a crystalline form I of atorvastatin hydrate in methanol containing water and stirring the same and (b) a step of isolating a crystalline form II of atorvastatin or a hydrate thereof or (a') a step of suspending a crystalline form I of atorvastatin hydrate in methanol and (b') a step of cooling and isolating a crystalline form IV of atorvastatin or a hydrate thereof.