Patent SG-11201804811W-A (SG)
Title: Fenfluramine compositions and methods of preparing the same
Inventor: LONDESBROUGH DEREK
IPC: B01J27/25
Filed: 2016-12-20
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -' Organization International Bureau ristsplid (43) International Publication Date .... ......r el 29 June 2017(29.06.2017) WIPO I PCT ID Hit (10) WO 111111111111111111IIIIIIII International II III 2017/112702 III IIIII Publication 111111111111 IIII Number Al RIO IIII IIIIIIII (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every B01J 23/72 (2006.01) B01J 27/25 (2006.01) kind of national protection available): AE, AG, AL, AM, B01J 27/055 (2006.01) CO7C 45/54 (2006.01) AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BOM 27/122 (2006.01) CO7C 49/223 (2006.01) BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (21) International Application Number: HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, PCT/US2016/067856 KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, (22) International Filing Date: MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 20 December 2016 (20.12.2016) NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, (25) Filing Language: English TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, (26) Publication Language: English ZA, ZM, ZW. (30) Priority Data: (84) Designated States (unless otherwise indicated, for every 62/271,172 22 December 2015 (22.12.2015) US kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, (71) Applicant: ZOGENIX INTERNATIONAL LIMITED TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, [GB/GB]; Siena Court Broadway, Maidenhead Berkshire TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, SL6 1NJ (GB). DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, (72) Inventors; and LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, (71) Applicants : LONDESBROUGH, Derek [GB/GB]; c/o SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, Zogenix International Limited, Siena Court Broadway, GW, KM, ML, MR, NE, SN, TD, TG). Maidenhead Berkshire SL6 1NJ (GB). ANDERSEN, Published: Marc W. 4500 Touchstone Forest Road, [US/US]; 21(3)) Raleigh, North Carolina 27612 (US). — with international search report (Art (74) Agent: FOULDS, Glenn J.; Bozicevic Field & Francis LLP, 201 Redwood Shores Parkway, Suite 200, Redwood City, California 94605 (US). Title: FENFLURAMINE AND METHODS PREPARING THE SAME (54) COMPOSITIONS OF 0 F OH Me 0 Me 0 Acetic Anhydride H 2 N Me Add (4) Ethy amine F 3 C le i 1-1 .4t ei O t--- ei 1-1 1-1 ---- (57) : Methods of preparing a fenfluramine active L 3 / 4 -- (a) hydrolyzing a 2-(3-(trifluoromethyl)phenyl)acetonitrile :::j position; (b) reacting the 2- (3-(trifluoromethyl)phenyl)acetic ei (3-(trifluoromethyl)phenyl)propan-2-one composition; and 0 composition with ethylamine using a borohydride reducing itions and pharmaceutical ingredients prepared according to fluramine and having less than 0.2% by weight in total of trifluoromethyl (c) FIG. pharmaceutical composition agent the (1 ) 1 ingredient are provided. Aspects of the method include to produce a 2-(3-(trifluoromethyl)phenyl)acetic acid com- acid composition with acetic anhydride and a catalyst to produce a 1- reductively aminating the 1-(3-(trifluoromethyl)phenyl)propan-2-one to produce a fenfluramine composition. Also provided are compos- subject methods including a pharmaceutically acceptable salt of fen- regioisomers.