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1. (WO2017060924) A NOVEL PIPECOLIC ACID CO-CRYSTAL OF CANAGLIFLOZIN AND PROCESS FOR THE PREPARATION THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2017/060924 International Application No.: PCT/IN2016/050344
Publication Date: 13.04.2017 International Filing Date: 08.10.2016
IPC:
C07D 409/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
10
linked by a carbon chain containing aromatic rings
Applicants:
HARMAN FINOCHEM LIMITED [IN/IN]; 07, Vinay Bhavya Complex 159 –A, C.S.T. Road, Kalina, Mumbai 400098 Maharashtra, IN
Inventors:
KADAM, Vijay Trimbak; IN
SAIKRISHNA, ,; IN
BHOSLE, Shrikrushna Ramrao; IN
MINHAS, Harpreet Singh; IN
MINHAS, Gurpreet Singh; IN
Agent:
P., Aruna Sree; IN
Priority Data:
3838/MUM/201509.10.2015IN
Title (EN) A NOVEL PIPECOLIC ACID CO-CRYSTAL OF CANAGLIFLOZIN AND PROCESS FOR THE PREPARATION THEREOF
(FR) NOUVEAU CO-CRISTAL D'ACIDE PIPÉCOLIQUE DE CANAGLIFLOZINE ET SON PROCÉDÉ DE PRÉPARATION
Abstract:
(EN) The present invention discloses the process for preparation of (2S,3R,4R,5S,6R)- 2-{3-[5-[4-Fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}-6- hydroxymethyl-tetrahydro-pyran-3,4,5-triol and its pipecolic acid co-crystal. The invention also discloses novel intermediate, acetic acid 4, 5-diacetoxy-6- acetoxymethyl-2-R1-2-{3-[5-(4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl- phenyl}-tetrahydro-pyran-3-yl ester, wherein, R1 is allyl or prop-2-ynyl, as an intermediate for the preparation of 4, 5-diacetoxy-6-acetoxymethyl-2-R1-2-{3-[5- (4-fluoro-phenyl)-thiophen-2-ylmethyl]-4-methyl-phenyl}-tetrahydro-pyran-3-yl ester, wherein, R1 is allyl or prop-2-ynyl.
(FR) La présente invention concerne un procédé de préparation de (2S,3R,4R,5S,6R)-2-{3-[5-[4-fluorophényl)-thiophén-2-ylméthyl]-4-méthylphényl}-6-hydroxyméthyl-tétrahydro-pyrane-3,4,5-triol et de son co-cristal d'acide pipécolique. Un nouvel intermédiaire, l'ester de 4,5-diacétoxy-6-acétoxyméthyl-2-R1-2-{3- [5-(4-fluorophényl)-thiophén-2-ylméthyl]-4-méthyl-phényl}-tétrahydro-pyran-3-yle d'acide acétique, où R1 est allyle ou prop-2-ynyle, est en outre décrit, à titre d'intermédiaire pour la préparation de l'ester de 4,5-diacétoxy-6-acétoxyméthyl-2-R1-2-{3-[5-(4-fluorophényl)-thiophén-2-ylméthyl]-4-méthylphényl}-tétrahydro-pyran-3-yle, où R1 est allyle ou prop-2-ynyle.
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, JP, KE, KG, KN, KP, KR, 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 (ARIPO) (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: English (EN)
Filing Language: English (EN)