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1. (WO2010078440) PROCESS AND INTERMEDIATES FOR THE PREPARATION OF N-ACYLATED-4-ARYL BETA-AMINO ACID DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/078440 International Application No.: PCT/US2009/069842
Publication Date: 08.07.2010 International Filing Date: 30.12.2009
IPC:
A01N 37/44 (2006.01) ,A61K 31/195 (2006.01)
A HUMAN NECESSITIES
01
AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
N
PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
37
Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
44
containing at least one carboxylic group or a thio-analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio-analogue of a carboxylic group, e.g. amino-carboxylic acids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
185
Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19
Carboxylic acids, e.g. valproic acid
195
having an amino group
Applicants:
CHIRAL QUEST, INC. [US/US]; 7 Deer Park Drive, Suite E Monmouth Junction, NJ 08852, US (AllExceptUS)
WU, Shulin [CN/US]; US (UsOnly)
YU, Bo [CN/CN]; CN (UsOnly)
WANG, Yejing [CN/CN]; CN (UsOnly)
DELICE, Alain [US/US]; US (UsOnly)
ZHU, Jingyang [US/US]; US (UsOnly)
Inventors:
WU, Shulin; US
YU, Bo; CN
WANG, Yejing; CN
DELICE, Alain; US
ZHU, Jingyang; US
Agent:
SHARAREH, Shahnam; Fox Rothschild LLP 997 Lenox Drive, Bldg. #3 Lawrenceville, NJ 08648, US
Priority Data:
61/142,03731.12.2008US
Title (EN) PROCESS AND INTERMEDIATES FOR THE PREPARATION OF N-ACYLATED-4-ARYL BETA-AMINO ACID DERIVATIVES
(FR) PROCÉDÉS ET INTERMÉDIAIRES DE SYNTHÈSE DE DÉRIVÉS D'ACIDES BÊTA-AMINÉS N-ACYLÉS-4-ARYLE
Abstract:
(EN) A process for producing an enantiomerically enriched, pure or enriched and essentially pure compound of Formula I [structure] wherein the R-, or S-configuration at the stereogenic center is marked with an *, which process hydrogenates an enamide compound of formula III [structure] in an organic solvent in the presence of a transition metal precursor complexed to a chiral phosphine ligand catalyst, wherein Ar is phenyl which is unsubstituted or substituted, R1 and R2 are selected from H, Cl - 8 alkyl, C5 - 12 cycloalkyl, aryl and aryl-C 1 - 2-alkyl, or R1 and R2 together with the nitrogen atom to which they are attached form a C4- r member heterocyclic πng system optionally fused with a 5- to 6- member carbocyclic or heterocyclic ring system, and the other substituents are as defined herein.
(FR) Procédé de production d'un composé énantiomériquement enrichi, pur ou enrichi et essentiellement pur de Formule I [structure] où la configuration R ou S du centre stéréogène est marquée d'une *, ledit procédé hydrogénant un énamide de formule III [structure] dans un solvant organique en présence d'un précurseur de métal de transition complexé à un catalyseur à ligands phosphine chiraux, Ar représentant un groupement phényle éventuellement substitué, R1 et R2 étant choisis parmi H, les groupements alkyle en C1-8, cycloalkyle en C5-12, aryle et aryl-(alkyle en C1-2), ou R1 et R2 forment ensemble et avec l'atome d'azote auxquels ils sont liés un système hétérocyclique à C4-r chaînons éventuellement fusionné à un système carbocyclique ou hétérocyclique à 5 ou 6 chaînons, et les autres substituants étant définis conformément au présent document.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP2381772CN102271504ES2603215IN2224/KOLNP/2011IN201838001902