Patent SG-11201808756X-A (SG)
Title: Process for the preparation of isoxazoline compounds
Inventor: YANG CHUNHUA
IPC: C07D453/04
Filed: 2017-04-05
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization 111111110111101110101011111010111110111010111111101111011111101111101111011111 International Bureau 0.. .... .. (10) International Publication Number (43) International Publication Date ..... ..or::,„, 12 October 2017(12.10.2017) WIPO I PCT WO 2017/176948 Al (51) International Patent Classification: (74) CO7D 261/04 (2006.01) A61K 31/42 (2006.01) Agent: JARECKI-BLACK, Judy; 3239 Satellite Blvd., Duluth, GA 30096 (US). CO7D 453/04 (2006.01) A61P 33/00 (2006.01) (81) Designated States (unless otherwise indicated, for every (21) International Application Number: PCT/US2017/026245 kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (22) International Filing Date: DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, 5 April 2017 (05.04.2017) HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (25) Filing Language: English KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, (26) Publication Language: English NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (30) Priority Data: 62/319,207 6 April 2016 (06.04.2016) US RU, RW, SA, 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. (71) Applicant: MERIAL, INC. [US/US]; 3239 Satellite Blvd., Duluth, GA 30096 (US). (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, — (72) Inventors: YANG, Chunhua; 20 Canady Ct., Belle Mead, NJ 08502 (US). LE HIR DE FALLOIS, Loic, Patrick; GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, 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, RS, SE, SI, SK, 2259 Fairhaven Circle NE, Atlanta, GA 30305 (US). MENG, Charles, Q.; 2291 Chance Lance, Grayson, GA 30017 (US). LONG, Alan; 5914 Stuart Drive, Flowery — Branch, GA 30542 (US). GORTER DE VRIES, Roelof, Johannes; 50 Avenue Marcel Merieux, 69290 St. Genis SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). — Les 011ieres (FR). BAILLON, Bruno; 9 Chemin de Pierre Grosse, 05300 Le Poet (FR). LAFONT, Sylvaine; 9 Rue Published: = des Romarines, Lieu dit les Salettes, 04160 Chat- — eau-Arnoux (FR). GAY DE SAINT MICHEL, Myriam; with international search report (Art. 21(3)) = 1 Chemin du Pra de L'Intra, 04310 Peyruis (FR). . KOZLOVIC, Stephane; 22 Rue du Bosquet, 04200 Sis- teron (FR). - = = Title: PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED ISOXAZOLINE COMPOUNDS - (54) = CRYSTALLINE TOLUENE SOLVATE OF (S)-AFOXOLANER = = I = on OBn 1_,Cf3 OH 0 NN Can Bn HN - • 1 H N _ —1 0 CF.3 .4 CF3 00 71' 01 IN Ci C 3 ilIA-11 ($)-aftarolluter 31 IN 31 CI0) (57) : This invention relates to processes for the preparation of antiparasitic isoxazoline compounds enriched in an enan - \" tiomer using quinine- based chiral phase transfer catalysts. The invention also relates to novel quinine-based phase transfer catalysts 0 and to a crystalline toluene solvate form of (S)-afoxolaner.