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1. (WO2018062799) METHOD FOR PREPARING (R)-N-[4-(1-AMINO-ETHYL)-2,6-DIFLUORO-PHENYL]-METHANESULFONAMIDE
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.:    WO/2018/062799    International Application No.:    PCT/KR2017/010582
Publication Date: 05.04.2018 International Filing Date: 26.09.2017
IPC:
C07C 303/44 (2006.01), C07C 311/08 (2006.01), B01D 9/00 (2006.01), A61K 31/18 (2006.01)
Applicants: AMOREPACIFIC CORPORATION [KR/KR]; 106, Hangang-daero, Yongsan-gu, Seoul 04386 (KR)
Inventors: WOO, Byoung Young; (KR).
LEE, Ki-Wha; (KR).
LEE, Jihae; (KR).
CHOI, Chang Soon; (KR).
PARK, Miyoung; (KR).
PARK, Young-Ho; (KR).
JAYAPRAKASH, Sarva; (IN).
REGATI, Sridhar; (IN).
SRINIVAS, Mamidi; (IN).
PATEL, Krushnakant; (IN).
RAMAMOHAN, M.; (IN)
Agent: KIM, Sun-young; (KR)
Priority Data:
10-2016-0124642 28.09.2016 KR
Title (EN) METHOD FOR PREPARING (R)-N-[4-(1-AMINO-ETHYL)-2,6-DIFLUORO-PHENYL]-METHANESULFONAMIDE
(FR) PROCÉDÉ DE PRÉPARATION DE (R)-N- [4- (1-AMINO-ÉTHYL) -2,6-DIFLUORO-PHÉNYL]-MÉTHANESULFONAMIDE
(KO) (R)-N-[4-(1-아미노-에틸)-2,6-다이플루오로-페닐]-메테인설폰아마이드의 제조방법
Abstract: front page image
(EN)Disclosed in the present specification is a method capable of preparing N-[4-[(1R)-1-[[(R)-(1,1-dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide (INT028-2) with high optical purity, through the selection of Ellman-chiral auxiliaries and the re-crystallization and separation of optical isomers. According to the above method, high-purity N-[4-[(1R)-1-[[(R)-(1,1- dimethylethyl)sulfinyl]amino]ethyl]-2,6-difluorophenyl]-methanesulfonamide with excellent quality can be produced at room temperature by improving cryogenic process conditions necessary for realizing high optical purity, and thus the trimming due to the process failure rate can be remarkably reduced.
(FR)La présente invention concerne un procédé permettant de préparer du N- [4- [(1R)-1-[[ (R)- (1,1-diméthyléthyl)) sulfinyl] amino] éthyl] -2,6-difluorophényl]-méthanesulfonamide (INT028-2) avec une pureté optique élevée, par la sélection d'auxiliaires d'Ellman-chiraux et la recristallisation et la séparation d'isomères optiques. Selon le procédé ci-dessus, du N- [4- [(1R)-1-[[ (R)- (1,1-diméthyléthyl)- (1,1-diméthyléthyl)) sulfinyl] amino] éthyl] -2,6-difluorophényl]-méthanesulfonamide avec une excellente qualité peut être produit à température ambiante en améliorant les conditions de traitement cryogénique nécessaires pour réaliser une pureté optique élevée, et, par conséquent, le rognage dû au taux de défaillance du processus peut être remarquablement réduit.
(KO)본 명세서에는 엘만 키랄 보조체의 선택성과 광학이성질체의 재결정 분리를 통해서, 높은 광학순도의 N-[4-[(1R)-1-[[(R)-(1,1-디메틸에틸)설피닐]아미노]에틸]-2,6-디플루오로페닐]-메탄설폰아미드(INT028-2)를 제조할 수 있는 방법이 개시된다. 상기 방법에 따르면 높은 광학순도를 구현하기 위해 필요한 극저온의 공정조건을 개선하여 상온에서 높은 순도의 N-[4-[(1R)-1-[[(R)-(1,1-디메틸에틸)설피닐]아미노]에틸]-2,6-디플루오로페닐]-메탄설폰아미드를 우수한 품질로 제조할 수 있으므로 공정 실패율에 따른 손질을 현저하게 감소시킬 수 있다.
Designated States: 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, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 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, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG).
Publication Language: Korean (KO)
Filing Language: Korean (KO)