Processing

Please wait...

Settings

Settings

Goto Application

1. WO2004005240 - PROCESS FOR PREPARING NATEGLINIDE AND INTERMEDIATES THEREOF

Publication Number WO/2004/005240
Publication Date 15.01.2004
International Application No. PCT/US2003/021238
International Filing Date 03.07.2003
Chapter 2 Demand Filed 03.02.2004
IPC
A61K 31/16 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
A61K 31/198 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-amino acids, e.g. alanine, edetic acid (EDTA)
C07C 51/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
51Preparation of carboxylic acids or their salts, halides, or anhydrides
58Preparation of carboxylic acid halides
60by conversion of carboxylic acids or their anhydrides into halides with the same carboxylic acid part
C07C 231/02 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
02from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/24 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
22Separation; Purification; Stabilisation; Use of additives
24Separation; Purification
C07C 233/63 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
233Carboxylic acid amides
57having carbon atoms of carboxamide groups bound to carbon atoms of rings other than six-membered aromatic rings
63having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
CPC
A61K 31/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
A61K 31/198
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
195having an amino group
197the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA],
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07C 231/02
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
02from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
C07C 231/24
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
231Preparation of carboxylic acid amides
22Separation; Purification; Stabilisation; Use of additives
24Separation; Purification
C07C 2601/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
2601Systems containing only non-condensed rings
12with a six-membered ring
14The ring being saturated
Applicants
  • TEVA PHARMACEUTICAL INDUSTRIES LTD. [IL]/[IL] (AE, AG, AL, AM, AT, AU, AZ, BA, BE, BF, BG, BJ, BR, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GW, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MZ, NE, NI, NL, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SI, SK, SL, SN, SY, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, YU, ZA, ZM, ZW)
  • TEVA PHARMACEUTICALS USA, INC. [US]/[US] (BB)
  • YAHALOMI, Ronit [IL]/[IL] (UsOnly)
  • SHAPIRO, Evgeny [IL]/[IL] (UsOnly)
  • DOLITZKY, Ben-Zion [IL]/[IL] (UsOnly)
  • GOZLAN, Yigael [IL]/[IL] (UsOnly)
Inventors
  • YAHALOMI, Ronit
  • SHAPIRO, Evgeny
  • DOLITZKY, Ben-Zion
  • GOZLAN, Yigael
Agents
  • BRAINARD, Charles R.
Priority Data
60/393,49503.07.2002US
60/396,90418.07.2002US
60/413,62225.09.2002US
60/414,19926.09.2002US
60/423,75005.11.2002US
60/432,09310.12.2002US
60/432,96212.12.2002US
60/442,10923.01.2003US
60/449,79124.02.2003US
60/479,01616.06.2003US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARING NATEGLINIDE AND INTERMEDIATES THEREOF
(FR) PROCEDE DE PREPARATION DE NATEGLINIDE ET DE SES INTERMEDIAIRES
Abstract
(EN)
Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with thionyl chloride in the presence of an effective amount of an organic amide. Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.
(FR)
La présente invention se rapporte à un procédé de préparation d'un intermédiaire utilisé pour la synthèse du natéglinide. Le chlorure d'acide trans-4-isopropylcyclohexane est formé par réaction d'acide 4- isopropylcyclohexanecarboxyle avec un chlorure de thionyle en présence d'une quantité efficace d'un amide organique. L'invention se rapporte également à des procédés pour la préparation de natéglinide par acylation d'un sel adapté de D-phenylalanine avec du chlorure d'acide trans-4-isopropylcyclohexane à la fois dans un système monophase et dans un système biphase, et dans de l'eau ne contenant pas de co-solvant.
Latest bibliographic data on file with the International Bureau