PROCESS FOR THE PREPARATION OF LEUKOTRIENE ANTAGONISTS

• Main Authors: VOLANTE RALPH P, BERGAN JAMES J, BHUPATHY MAHADEVAN, MCNAMARA JAMES M, SIDLER DANIEL R
• Format: Patent
• Language: English; Romanian
• Published: 27.02.2004
• Edition: 7
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; 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

The invention relates to a process for the preparation of leukotriene antagonists corresponding to the formula I and the sodium salts thereof, wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, process which supposes : reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropane acetic acid with a compound of formula (II), wherein HET is as defined above, and L is either arylsulfonyl or alkylsulfonyl. The invention relates to dicyclohexylamine salt of a compound of formula (I), to an intermediate of formula (II) and to a 1-(mercaptomethyl) cyclopropane acetic acid intermediate. Invenţia se referă la un procedeu pentru prepararea antagoniştilor de leucotrienă ce corespund formulei I, şi a sărurilor de sodiu ale acestora, unde HET este reprezentat de 7-clorochinolin-2-il sau de 6,7-difluorochinolin-2-il, procedeu ce presupune reacţia dianionului de dilitiu din acidul 1-(mercaptometil)ciclopropanacetic cu un compus având formula II, unde HET este conform descrierii anterioare, iar L este fie arilsulfonil, fie alchilsulfonil. Invenţia se referă şi la sarea de diciclohexilamină a compusului cu formula I, la un intermediar cu formula II şi la un intermediar al acidului 1-(mercaptometil)ciclopropanacetic. ŕ