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1. (WO2018127762) AN IMPROVED PROCESS FOR THE PREPARATION OF RIVAROXABAN INVOLVING NOVEL INTERMEDIATE
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Pub. No.: WO/2018/127762 International Application No.: PCT/IB2017/058245
Publication Date: 12.07.2018 International Filing Date: 21.12.2017
IPC:
A61K 31/422 (2006.01) ,A61K 31/5355 (2006.01) ,A61K 31/5377 (2006.01) ,A61P 7/02 (2006.01) ,C07D 413/14 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
41
having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
42
Oxazoles
422
not condensed and containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5355
Non-condensed oxazines containing further heterocyclic rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
5377
not condensed and containing further heterocyclic rings, e.g. timolol
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
7
Drugs for disorders of the blood or the extracellular fluid
02
Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
Applicants:
UNICHEM LABORATORIES LTD [IN/IN]; Unichem Bhavan, Prabhat Estate Off. S. V. Road, Jogeshwari (W), Mumbai Maharashtra 400102, IN
Inventors:
SATHE, Dhananjay G.; IN
DAS, Arijit; IN
RAIKAR, Sanjay; IN
SURVE, Yashwant S.; IN
PANDIT, Bhushan S.; IN
Agent:
KHURANA & KHURANA, ADVOCATES & IP ATTORNEYS; E-13, UPSIDC, Site-IV, Behind-Grand Venice Kasna Road, Greater Noida, National Capital Region, Uttar Pradesh 201310, IN
Priority Data:
20172100035104.01.2017IN
Title (EN) AN IMPROVED PROCESS FOR THE PREPARATION OF RIVAROXABAN INVOLVING NOVEL INTERMEDIATE
(FR) PROCÉDÉ AMÉLIORÉ POUR LA PRÉPARATION DE RIVAROXABAN IMPLIQUANT UN NOUVEL INTERMÉDIAIRE
Abstract:
(EN) The present invention relates to the novel key intermediate, 4-{4-[(5S)-(Aminomethyl)-2- oxo-l,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, in the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
(FR) La présente invention concerne le nouvel intermédiaire clé perchlorate de 4-{4-[(5S)-(aminométhyl)-2- oxo-1,3-oxazolidin-3-yl]-phényl}-morpholin-3-one dans la synthèse du rivaroxaban. L'invention concerne en outre la forme cristalline d'un nouvel intermédiaire, le procédé pour préparer le nouvel intermédiaire et un procédé de préparation de rivaroxaban à l'aide de ce nouvel intermédiaire. L'invention concerne un procédé amélioré et efficace pour la préparation de rivaroxaban.
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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, 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 Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (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)