Patent SG-11201805595T-A (SG)
Title: Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1h-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid
Inventor: CHEN JUNLI
IPC: C07D487/04
Filed: 2017-02-16
Abstract: INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization M1111101110101011111 HO 11111 011101011101110111 100 II0 In III 11 International Bureau .. .... ..Yejd .... ...,,, (10) International Publication Number (43) International Publication Date WO 2017/140750 Al 24 August 2017 (24.08.2017) WI P0 I P CT (51) International Patent Classification: (72) Inventor: CHEN, Junli; Building No. 5, Lane 720 Cailun C07D 487/04 (2006.01) Road, Shanghai 201203 (CN). (21) International Application Number: (74) Agent: HALBIG, Dirk; Grenzacherstrasse 124, 4070 PCT/EP2017/053443 Basel (CH). (22) International Filing Date: (81) Designated States (unless otherwise indicated, for every 16 February 2017 (16.02.2017) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (25) Filing Language: English BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, (26) Publication Language: English DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, (30) Priority Data: KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, PCT/CN2016/074132 MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, 19 February 2016 (19.02.2016) CN NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, (71) Applicant (for all designated States except US): F. HOFF- RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, MANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 124, 4070 Basel (CH). ZA, ZM, ZW. (71) Applicant (for US only): HOFFMANN-LA ROCHE (84) Designated States (unless otherwise indicated, for every INC. [US/US]; Overlook at Great Notch, 150 Clove Road, kind of regional protection available): ARIPO (BW, GH, 8th Floor, Suite 8 - Legal Department, Little Falls, New GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, — Jersey 07424 (US). TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, — TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, = = [Continued on next page] = (54) Title: = IC ACID = = 2 = = = = = .4 © kin IN © ii- ,—, IN ,—, © ei 0 C N PROCESS FOR HO B O 1 \ R 1 - - R 3 = HYDROPYRIMIDIN-6-YLNETHYL]-3-0X0-5,6,8,8A-TETRAHYDRO-1H-IMIDAZO THE N _ R.,... PREPARATION OF 4-PHENYL-5-ALKOXYCARBONYL-2-THIAZOL-2-YL-1,4-DI- [1,5-A]PYRAZIN-2-YL]-CARBOXYL - (57) : The present invention relates to a process for synthesizing a compound of formula (I), R 1 is phenyl, which is unsubstituted or substituted with one, two or three substitu- ents independently selected from halogen and C alkyl; R i _ 6 2 is C alkyl; R i _ 6 3 is -C,,H2.-; x is 1, 2, 3, 6 or 7; or pharmaceutic- ally acceptable salt or diastereomer thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepat- itis B infection. (I) O WO 2017/140750 Al MIDEDIMOHNIIMMEOMMEIMMINEMOVOIMIE DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, Published: LU, LV, MC, MK, MT, NL, PL, PT, RO, RS, SI, SK, SM, TR), OAPI (BF, CF, CG, CI, CM, GN, GQ, GW, KM, ML, MR, NO, BJ, NE, SN, TD, TG). SE, GA, with international search 21(3)) report (Art. Declarations under Rule 4.17: — of inventorship (Rule 4.17(iv))